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B i o t e c h G m B hIris

From Grams to multI -ton lots

EdItIon 2012

ComprEhEnsIvE druG dElIvEry survEy

a directory of all Currently available drug Carrier and drug delivery systems

pGa – pEGylation – pasylation – dendrimers

Iris BIotech | coMPReheNSIVe DRUG DeLIVeRY SURVeY

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From Grams to Multi-Ton Lots

3IRIS BIotech GMBh WeB WWW.IRIS-BIotech.De MAIL [email protected] teL +49 9231 96 19 73 FAX +49 9231 96 19 99


coNteNt

Introduction ........................................................................................................5

1. Basics and Principles of Polymer therapeutics .............................................. 81.1 Pharmacological Effects in Polymer Therapeutics .................................................................................... 81.2 Polydispersity .......................................................................................................................................... 101.3 Comparison of Different Polymer Therapeutic Technologies ................................................................... 11

1.3.1 PGA – Poly(glutamic acid) –

a Drug Carrier with low Polydispersities and Versatile Architectures ....................................... 12

1.3.2 PEG – Poly(ethylene glycol) ...........................................................................................................17

1.3.3 PASylation Technology ................................................................................................................. 19

1.3.4 Dendrimers .................................................................................................................................. 21

2. Available PGA - Poly(glutamic acid) Derivatives ............................................242.1 Poly(glutamic acid) Base Polymers .........................................................................................................24

2.1.1 Alkyl Terminated PGA ...................................................................................................................24

2.1.2 Click Terminated PGA ................................................................................................................. 262.2 Poly(glutamic acid) Copolymers ........................................................................................................... 28

2.2.1 Alkyl Terminated Click-PGA Copolymer ...................................................................................... 28

2.2.2 Alkyl Terminated mPEG-PGA Co-Polymer ...................................................................................37

2.2.3 Click Terminated mPEG-PGA Co-Polymer ....................................................................................39

3. Available monodisperse, polydisperse and branched PeGylating Reagents...423.1 Branched PEGylating Reagents ..............................................................................................................423.2 Amino-PEG-Acids and Active Esters ...................................................................................................... 46

3.2.1 Aloc Protected Amino-PEG-Acids .................................................................................................47

3.2.2 Boc Protected Amino-PEG-Acids ................................................................................................ 48

3.2.3 Dde Protected Amino-PEG-Acids ................................................................................................. 51

3.2.4 Dnp Protected Amino-PEG-Acids .................................................................................................52

3.2.5 Fmoc Protected Amino-PEG-Acids ...............................................................................................53

3.2.6 Mtt and Mmt Protected Amino-PEG-Acids ..................................................................................57

3.2.7 N-Unprotected Amino-PEG-Acids and Esters .............................................................................. 59

3.2.8 Z Protected Amino-PEG-Acids .................................................................................................... 643.3 PEG-Acids carrying various other Terminal Groups ...............................................................................65

3.3.1 Formyl-PEG-Acids .........................................................................................................................65

3.3.2 Acryloyl-PEG-Acids ......................................................................................................................65

3.3.3 Epoxy-PEG-Acids......................................................................................................................... 66

3.3.4 Hydroxy-PEG-Acids ..................................................................................................................... 66

3.3.5 PEG-Di-(Carboxylic Acids) ........................................................................................................... 68

3.3.6 mPEG- and other Alkyl-PEG-Acids, Esters and Carbamates ........................................................73

3.3.7 Dye labeled PEG-Acids ................................................................................................................. 773.4 PEG-Amines, Hydrazines, Guanidines .................................................................................................... 77

3.4.1 Mono Protected PEG-diamines .................................................................................................... 77




3.4.2 Unprotected PEG-diamines ........................................................................................................ 80

3.4.3 Amino-PEG-alcohols .................................................................................................................... 81

3.4.4 mPEG-amines ..............................................................................................................................833.5 PEG-Alkynes&Azides for Click-Chemistry .............................................................................................. 86

3.5.1 PEG-Alkynes .................................................................................................................................87

3.5.2 PEG-Azides ..................................................................................................................................923.6 Biotin-PEG Reagents .............................................................................................................................1003.7 PEG-Thiols .............................................................................................................................................. 111

3.7.1 Lipoamide-PEGs ........................................................................................................................... 111

3.7.2 Mercapto-PEG-Acids .................................................................................................................... 116

3.7.3 Amino- and Hydrazido-PEG-Thiols ..............................................................................................124

3.7.4 Methoxy-PEG-Thiols ................................................................................................................... 126

3.7.5 Hydroxy-PEG-Thiols .................................................................................................................... 128

3.7.6 Bis-Mercapto-PEG ....................................................................................................................... 1303.8 PEG-Maleinimides ................................................................................................................................. 131

3.8.1 Non-PEG Maleinimido-Acid-Crosslinkers .................................................................................... 131

3.8.2 Maleinimido-PEG-Acids..............................................................................................................132

3.8.3 Maleinimido-PEG-Amines and Hydrazides ............................................................................... 136

3.8.4 Methoxy-PEG-Maleinimides ......................................................................................................137

3.8.5 Bis-Maleinimido-PEGs ............................................................................................................... 1393.9 PEG-Silanes .......................................................................................................................................... 1403.10 Other PEG Reagents ............................................................................................................................ 142

3.10.1 Bromo-PEGs .............................................................................................................................. 142

3.10.2 Bishydroxy-PEGs ...................................................................................................................... 143

3.10.3 Methoxy-PEG-Alcohols ............................................................................................................. 144

3.10.4 PEG-Aldehydes ......................................................................................................................... 146

4. Available Dendrimers and Dendron Building Blocks ................................... 1484.1 Available PEG based Dendrimers ......................................................................................................... 1484.2 Available 2,2-bis(hydroxymethyl) propionic acid based Dendrons ..................................................... 150

4.2.1 Azido Dendrons ......................................................................................................................... 150

4.2.2 Alkyne Dendrons ...................................................................................................................... 152

4.2.3 Allyl Dendrons ...........................................................................................................................153

4.2.4 Disulfide bridged Dendrons .................................................................................................... 155

4.2.5 PEG bridged Dendrons ..............................................................................................................157

5. Index ........................................................................................................... 158

6. terms and conditions of Sales .....................................................................170




Proteins and other Biopharmaceuticals have a high poten-tial as drugs due to their specificity and efficacy, but show poor pharmacokinetic properties. Attaching polymers, which are tolerated by the physiologic system, such as PGA (poly(glutamic acid)), PEG (poly(ethylene glycol)) or PAS (random polypeptide of proline, alanine and serine) improves drastically their bioavailability and biodistribu-

tion and turns sensitive biomolecules into robust drugs.

In 2006 the market of modern biopharmaceuticals has reached a volume of over $45 billion per year world wide (IMS Health, Inc.) and has been grown significantly. The big advantage of proteins, antibodies, siRNA, and other natural products in their usage as drugs is their high specificity in combination with their low side effects. Normally they interact with the dedicated target only, and thus do not show unwanted activities and side effects at any other place in the body. A current focus is the study of modern drug carrier systems where biotolerable linkers are connecting a recognition part with a drug-active part. Conjugations can reach the size of a nanoparticle. The rec-ognition part can be a peptide or hormone, which binds specifically to the surface of a certain cell. After internal-ization of the whole nanoparticle the active part (DNA or siRNA, for example) is released. Inhibition or activation of certain enzymes or the nucleus follows with the conse-quence to repair the sick cell, to shut it down by initiating apoptosis or other mechanisms. Is the recognition part somehow specific to a certain individual, the drug system becomes personalized (“Personalized Medicine”). In conjugation with hydrophobic compounds forming amphi-philic and biodegradable block-copolymers like PEG-PLA (polylactic acid) and PEG-PLGA (co-polylactic acid-glycolic acid) sophisticated micelles are formed, where drug mol-ecules can be masked and protected against attacks by the immune system.

Modern biopharmaceuticals are ideal drugs. However,

their significant drawback is their low stability under physiological conditions. Due to the fact that they are similar to biological components, they are also eas-ily attacked by the immune system of the body, i.e. by antibodies and proteolytic degradation enzymes. Many efforts have been made by highly sophisticated formula-tion techniques, special application methods (depots) and chemical modifications to improve their pharmacokinetic properties. One approach, which shows much better results than other methods tried in the past, is Polymer Therapeutics, i.e. attaching polymers to the active compo-nent. One possibility is attaching a monofunctional PEG chain to a protein, antibody or small drug molecule. Using bifunctional PEGs a linkage between two compounds can be formed, in order to build dimers or more complex conjugates.

There has been a permanent search for new types of polymers going on, in order to enlarge the field of Polymer Therapeutics to new classes of drug molecules. One interesting group are poly amino acids consisting of one amino acid as monomer. Typical examples are polylysine and poly(glutamic acid), polymers, which don’t exist in nature, but show good physiological properties, due to their similarity to natural proteins. PGA - poly(glutamic acid) has been identified as suitable carrier system. PGA shows the ability to conjugate with partners on N- and C-terminus, analogue to alpha and omega derivatisation of a PEG – poly(ethylene glycol). Additionally and in fact the way, it is mostly used so far, is to use the glutamic acid side chains for forming any carbonyl function, like esters and amides. The number of side chains naturally is very high compared to only one N- and C-terminus in one chain. Therefore a multiple loading to the polymer chain is possible. With PGA therefore, the polymer therapeutics effect can also be applied to small drug molecules. It is theoretically also possible to PEGylate a small molecule. However, mostly inactivation of the small drug molecule is the consequence. PGA therefore is an ideal carrier in particular for APIs with low molecular weight.

PEGylated Enzyme

PEGylated Peptide

Introduction




PGA, PEG and PAS are polymers lining up each of their monomers in one row. Since long there have been made efforts to design large molecules with building blocks of higher valency (trivalent and higher), in order to build up a three-dimensional highly branched construct. Polyly-sine, as a typical example, has already been used for

immunogenic applications since decades. This so called dendrimers and dendrons are monodisperse and usually highly symmetric, spherical compounds. Their properties are dominated by the functional groups on their outer shell. Dendrimers are classified by generation, which refers to the number of repeated branching cycles that are performed during their synthesis.

Applications of dendrimers typically involve conjugating other chemical species to the dendrimer surface that can function as detecting agents (such as a dye molecule) in diagnostic applications, affinity ligands, targeting compo-nents, radioligands, imaging agents, or pharmaceutically active compounds. Dendrimers have very strong potential,

because their structure leads to multivalent systems. In other words, one dendrimer molecule has many of pos-sible sites to couple to an active species. The majority of drugs available in pharmaceutical industry are hydropho-bic in nature and this property in particular creates major

References:

f Modulation of Cellular Apoptosis with Apoptotic Protease-Activation

Factor 1 (Apaf-1) Inhibitors; L. Mondragón, M. Orzáez, G. Sancli-

mens, A. Moure, A. Armiñán, P. Sepúlveda, A. Messeguer, M. J.

Vicent, E. Pérez-Payá; J. Med. Chem. 2008; 51: 521-529.

f Integrin-assited drug delivery of nano-scaled polymer therapeutics

bearing paclitaxel; Anat Eldar-Boock, Keren Miller, Joaquin Sanchis,

Ruth Lupu, Maria J. Vicent, Ronit Satchi-Fainaro; Biomaterials 2011;

32: 3862-3874.

NH

O

OO

HN

HN

O

NH

HN

O

O

O- Na+O

Drug

PGA

O- Na+O O- Na+O

PGA PGA

PGA Peptide Conjugate

First generation pentavalent PEG based dendrimer with five identical reactive groups.

First generation pentavalent PEG based dendrimer with three different reactive groups, for example Click reactive, carboxylic acid (amine reactive) and protected amine (nucleophilic).




formulation problems. This drawback of drugs can be upgraded by hydrophilic dendrimeric scaffolding.

Examples in drug delivery applications combine dye mol-ecules and a strand of DNA on the same dendrimer. Ap-proaches for delivering unaltered natural products using polymeric carriers are of widespread interest. Dendrimers have been explored for the encapsulation of hydrophobic compounds and for the delivery of anticancer drugs. The physical characteristics of dendrimers, including their monodispersity, water solubility, encapsulation ability, and large number of functionalizable peripheral groups, make these macromolecules appropriate candidates for evaluation as drug delivery vehicles. Dendrimers have been explored for controlled delivery of antiretroviral bio-actives. The inherent antiretroviral activity of dendrimers enhances their efficacy as carriers for antiretroviral drugs. These encouraging results of current examples provide further impetus to design, synthesize, and evaluate new dendritic polymers for use in basic drug delivery studies and eventually in the clinic.

References:

f Tathagata Dutta and N.K. Jain. Targeting Potential and Anti HIV

activity of mannosylated fifth generation poly (propyleneimine)

Dendrimers. Biochimica et Biophysica Acta 2007; 1770: 681-686.

f Tathagata Dutta, Minakshi Garg, Narendra K. Jain. Targeting of Efa-

virenz Loaded Tuftsin Conjugated Poly(propyleneimine) dendrimers

to HIV infected macrophages in vitro. Eur. J. Pharm. Sci. 2008;

34(2-3): 181-189.

f Tathagata Dutta, Hrushikesh B. Agashe, Minakshi Garg, Prahlad

Balakrishnan, Madhulika Kabra, Narendra K. Jain. Poly (propylenei-

mine) dendrimer based nanocontainers for targeting of efavirenz to

human monocytes/macrophages in vitro. Journal of Drug Targeting.

2007; 15(1): 84-96.

f Cheng, Yiyun; Qinglin Wu, Yiwen Li, Tongwen Xu. External Electro-

static Interaction versus Internal Encapsulation between Cationic

Dendrimers and Negatively Charged Drugs: Which Contributes

More to Solubility Enhancement of the Drugs?. Journal of Physical

Chemistry B 2008; 112(30): 8884–8890. doi:10.1021/jp801742t. PMID

18605754.

Second generation dendrimer based on a pentavalent PEG based building block for sophisticated applications in drug delivery, diagnostics, combination therapy or personalized medicine.

Each of the polymer technologies mentioned above has its inherent properties and advantages. The following sections compare the different characteristics of each carrier system and explain properties and applications in detail. We hope that with this survey the selection of the right carrier system will become easier to the user.




1. Basics and Principles of Polymer therapeutics 1.1 Pharmacological effects in Polymer therapeutics

0 1 2 3 4 5 6 7 8

0 24 48 72 96 120 144 168 192 216 240

Conc

entr

atio

n in

the

Bod

y

Time [h]

Pharmacokinetic properties of a PEGylated drug in comparison to a non PEGylated drug.

Single Application of a PEGylated Drug

Often and Repeated Treatment of a non-PEGylated Drug

Single Dose of a non-PEGylated Drug

the Reasons, why Polymer Therapeutics improves Drug Delivery and PharmacokineticsSmall drug molecules and also large biomolecules like proteins or antibodies suffer rapid clearance in human body. The concentration of the drug compound drops rapidly as it is removed from the body. Treatment has to be repeated, in order to keep the concentration over the therapeutic threshold. Otherwise immunogenic reactions start. PEGylated drugs show suppressed renal clearance and reduced immunogenic reactions, the concentration is being reduced only very slowly over the time of treatment. In the ideal case only a single application is required over the time of treatment.

this is due to the following two mechanisms:1) Preventing Degradation and Reducing ImmunogenicityThe polymer chains are covering the surface of a biophar-maceutical and thus effectively shielding it against attacks by the immune system. The polymeric shield has charac-teristics rather like a solvent than a protein.

This prevents uptake by cells of the retinal endothelial system (macrophage system). Recognition by the immune system (antibodies, proteases and other degradation en-zymes etc.) is significantly reduced. The drug stays intact and is not destroyed (degraded or metabolized) during its presence in the body and journey through the physiologi-cal system.

2) Preventing ExcretionPGA, PEG and PAS are naturally very hygroscopic and sur-rounded by a large solvating sphere with water. Thus the overall so-called “hydrodynamic radius” has increased to an order of magnitude, which is larger than the diameter of the glomerular capillaries (6 to 12 nm). Therefore the drug is not excreted through the kidneys and simply stays longer in the body.

Retarded renal filtration prolongs plasma half-life of the biological drug by means of a purely biophysical size ef-fect, without any receptor interactions that may influence pharmacodynamics or lead to side effects.

These two main effects, i.e. preventing degradation and excretion, lead to a set of advantegous properties of polymer therapeutic drugs. The polymer forms a ran-dom conformation which is stable under native buffer conditions and body temperature and generates a large hydrodynamic volume, thus increasing the apparent size. Through the choice of different chain lengths and polymer design the hydrodynamic volume can be adjusted within broad limits.




table: PeG conjugates in the pharmaceutical market*Conjugate Trade Name Indication Year to Market

PEG-adenosin deaminase Adagen® 1990

PEG-L-asparaginase Oncaspar® Acute lymphoblastic leukaemia 1994

PEG-interferon α2b PEG-INTRON® Hepatitis C (cancer, MS, HIV) 2000

PEG-interferon α2a PEGASYS® Hepatitis C 2002

PEG-growth hormone receptor antagonist Pegvisomant® Acromegaly 2002

PEG-G-CSF PEG-filgrastim®, Neulasta® Treatment of neutropaenia during chemotherapy 2002

PEG-anti-VEGF aptamer Pegaptanib®, Macugen® Macular degeneration 2004

PEG-anti TNF Fab CD870® Rheumatoid arthritis 2005

PEG-aspargase Oncaspar® Acute lymphoblastic leukaemia 2006

f * A) Duncan, Ruth, The Dawning Era of Polymer Therapeutics, Nature Reviews Drug Discovery 2003; 2: 347-360. B) Veronese, Francesco, M.

PEGylation, successful approach to drug delivery, Drug Discovery Today 2005; 10(21): 1451-1457.

hydrodynamic radius of a PEGylated drug compound

Additional References, Books and Review Articles:

f Bruckdorfer, Th.; PEGylation – The Magic Wand – Turning Proteins

and other Biopharmaceuticals into Super Performing Block Busters;

PharManufacturing 2007; 34-41.

f Schiffelers, R.M., Ansari, A., Xu J., Zhou, Q., Tang, Q., Storm, G.,

Molema, G., Scaria, P.V., Woodle, M.C.; Cancer siRNA therapy by

tumor selective delivery with ligand-targeted sterically stabilized

nanoparticle; Nucleic Acid Research 2004; 43(19): 149.

f Ogris, M., Walker, G., Blessing, Th., Kircheis. R., Wagner, E.; Tumor-

targeted gene therapy: strategies for the preparation of ligand-

polyethylene glycolpolyethyleneimine- DNA complexes, Journal of

Controlled Release 2003; 91: 173-181.

f Trimaille, Th., Mondon, K., Gurny, R., Möller, M.; Novel polymeric

micelles for hydrophobic grug delivery based on biodegradable

poly(hexyl-substitude lactides); International Journal of Pharmaceu-

tics 319 2006; 319: 147-154.

f Chapman, Andrew, P. PEGylated antibodies and antibody fragments

for improved therapy: a review; Advanced Drug Delivery Reviews

2002; 54: 531-545.

f Roberts, M.J., Bentley, M.D., Harris, J.M.; Chemistry for peptide and

protein PEGylation; Advanced Drug Delivery Reviews 2002; 54:

459-476.

f Veronese, Francesco M. Peptide and protein PEGylation: a review of

problems and solutions, Biomaterials 2001; 22: 405-417.

f Bückmann A. et al.; Makromol. Chem. 1981; 182: 1379.

f Pillaia V.N. et al., J. Org. Chem. 1980; 45: 5364.

f Harris J.M. et al., J. Polym. Sci. Polym. Chem. Edn. 1984; 22: 341.

f Zalipski S. et al., Eur. Polym. J. 1983; 19: 1177.

f Abuchowski A. et al., J. Biol. Chem. 1977; 252: 3578.

f Cordes A. et al., J. Chromat. 1986; 376: 375.

f Wirth P. et al., Bioorg. Chem. 1991; 19: 133.

f Kogan T.P., Synthetic Comm. 1992; 22: 2417.

the glomerular capillaries have a cross section of 6 – 12 nm




1.2 Polydispersity The polymers in this context (PGA, PEG, PAS) are a poly-meric linear structure with n repeating units of mono-mers. Depending, whether the polymer is consisting of one single molecular weight (only one n existing) or of a range of compounds with an average mass and a distribu-tion of n around a mean value, polymers are referred to as “monodisperse” or “polydisperse”. If the polymer is polydisperse it shows a mass spectrum as shown in the figure. In order to quantify the distribution of the molecu-lar weight the Polydispersity D is defined as the ratio between the weight average molecular weight M

w° and

the number average molecular weight Mn°. The weight

average molecular weight does not “count” species just by their number, but takes into account the total weight of each species and is therefore a much more realistic indicator of the gross mechanical property. For a homo-geneous sample, where the polymer chains have all the same length, M

w° is equal to M

n°, the polydispersity D is

then equal to 1 and the sample is referred to be monodis-perse.

Whenever there is a distribution of molecular weights, the weight average M

w° is always greater than the num-

ber average Mn° and the polydispersity is greater than 1.

The polydispersity D of PEGs and PGAs typically used in polymer therapeutics is between 1.05 and 1.20. Though, whenever a PEGylated new drug compound needs to be approved by EMEA, FDA and other authorities, it is easier and faster, if this compound shows only one signal in the mass spectrum and not a distribution pattern. Therefore the need for high molecular weight, but monodisperse compounds is increasing. PAS polymers are the choice in this case. As they are produced through recombinant methods, only one specific molecular weight exists, although it is a large molecule.

Reference:

f Painter, P.C., Coleman, M.,M.; Fundamentals of Polymer Science,

ISBN 1-56676-559-5, CRC Press, 1997; 22.

Poly(ethylene glycol) is a polymeric linear structure with repeating polyethylene oxide units.

Mass spectrum of a polydisperse polyethylene glycol showing the typical signals with a difference of: m/z = 44

Whenever there is a distribution of molecular weights, the weight average M

w° is always greater than the number

average Mn° and the polydispersity D is greater than 1.

D = ≥ 1 with Mw

° = and Mn° =

Mw

° Σ Nx M

x

2 Σ Nx M

x

Mn° Σ N

x M

xΣ N

x




Parameter PGA PEG PAS Dendrons

Monomer glutamic acid ethylene glycol proline, alanine and serine different

Polydispersity D = 1.1 – 1.2 monodisperse for short PEGs: D = 1

PEGs with MW 1 kDa: D = 1.05 – 1.25

Strictly monodisperse

D = 1

D ~ 1

Molecular Weight

1 kDa ~ 100 kDa 100 Da - 20 kDaapplications published with 40 kDa and 60 kDa

by design 100 Da ~ 4 kDa

Biocompatibility biocompatible and biode-gradable by thiol protease cathepsin B for any molecu-lar weight

FDA approved; non-antigenic and non-immuno-genic certainly up to 20 kDa

however, toxicity through accumulation in the liver observed for PEGs with MW > 60 kDa;

high doses generate lysosomal storage disease

biocompatible and biode-gradable by proteases at any molecular weight

depending on monomer

Application biopharmaceuticals;

special advantage for small molecules;

multiple loading can also be used for immunogenic applications;

small PEGs show only improvement in solu-bilty, no special polymer therapeutic effect;

longer PEGs are very widely used with large molecules and biopharmaceuticals

in particular useful and de-veloped for biopharmaceu-ticals, whose expression system can be modified for PAS coexpression

small molecules; multiple loading can also be used for immunogenic applications.

Conjugation Technique

chemical synthesis chemical synthesis recombinant synthesis only;

reagents for chemical synthesis in preparation

chemical synthesis

# of conjugation partners

multivalent bivalent monovalent multivalent

Chemical Versatility

commercially available with a certain set of functional groups:

click conjugation;

amine reactive;

other derivatives can easily be constructed and are in development

commercially available with a very large variety of functional groups:

click conjugation;

amine and carboxy reactive;

thiol and maleinimide;

many biotin derivatives;

aldehydes;

silanes and many others

amine and carboxylic reactive;

difficult to construct other functionality

larger variety of functional groups available depending on the dendrimer monomer

1.3 comparison of Different Polymer therapeutic technologies

Dendrimer

PEG

PGA

PAS

Each polymer carrier technology has its characteristics and strong points for certain application fields. We hope that with this survey, we can make the decision for potential

users easier to select the right polymer for the given drug molecule or application.




Polyglutamates are well known to be highly biocompat-ible, biodegradable and multifunctional polymers, which have already been used as building blocks in polymer drug conjugates and polymeric micelles. Those systems have been applied to various medical applications ranging from therapy to molecular imaging. Furthermore a PGA paclitaxel conjugate has already entered clinical stud-

ies (OpaxioTM PGA-paclitaxel (PTX) conjugate currently in phase III of clinical trials). In this context, a synthetic path-way to a plethora of functional polyglutamates (homo-polymers, block-co-polymers) with well-defined structure, adjustable molecular weight (Mw) and low dispersity (D = Mw/Mn <1.2) applying the ring opening polymeriza-tion (ROP) of N-carboxyanhydrides (NCA) are offered. Additionally, as the acid moieties of the polyglutamates can be activated, various functionalities were introduced by “post-polymerization modification” yielding a set of orthogonal reactive side chains. The reactive moieties, such as azides, maleimides, thiols, or alkynes offer the opportunity of specific conjugation of drugs, targeting moi-eties or markers.

Besides introducing reactive groups the functionalization strategy has also been used for PEGylation of PGA. This modification could reduce charge induced interactions and therefore change pharmacological properties, such as blood circulation.

In summary, a tool kit of various polyglutamates is offered enabling the synthesis of a variety of polymer drug con-jugates or polymer based imaging agents. The functional polymeric precursors offered allow functionalizing and therefore adjusting the polymer properties to a desired application.

Background information:

An ideal polymer to be used as carrier for drug delivery or molecular imaging should be characterized by

1. biodegradability or adequate molecular weight that allows elimination from the body to avoid progressive accumulation in vivo;

2. low polydispersity, to ensure an acceptable homoge-neity of the final system allowing to adjust pharmaco-kinetics;

3. longer body residence time either to prolong the conjugate action or to allow distribution and accumu-lation in the desired body compartments (therefore high molecular weight is desired);

4. and for small drug conjugation, by availability of many reactive groups, in order to achieve a satisfac-tory drug loading or to allow polymer-based combina-tion therapy (multivalent polymers).

Most polymer conjugates in the market and in the clinics use N-(2-hydroxypropyl)methacrylamide (HPMA) co-polymers, PEG or more recently polyglutamic acid (PGA) as carriers. Biopersistent carriers (PEG, HPMA) present disadvantages, if chronic parenteral administration and/or high doses are required as there is the potential to gener-ate ‘lysosomal storage disease’ syndrome. Alternatively, polyglutamates are well known to be highly biocompat-ible, biodegradable (by thiol protease cathepsin B) and multifunctional polymers, which have been already ap-plied to various applications that range from drug delivery systems, tissue engineering, sensing, and catalysis. PGA is considered a promising material for the design of novel nanomedicines due to its high biocompatibility, multiva-lency and in vivo degradability. As a prominent example for their use as nanopharmaceutical, one has to mention a conjugate of polyglutamic acid (PGA) and paclitaxel (OpaxioTM, formerly Xyotax, PPX, CT-2103) in phase III of clinical trials. Another clinical example is provided by several polymeric micelles – firstly developed by Kataoka – that were designed based on the block-copolymer PEG-PGA, namely NK 105, NK-6004, Nanoplatin or NC-4016 in Phase I-II trials. Other recent examples of the use of this multifunctional, biodegradable polyanionic carrier can be found in many drug delivery applications not only in cancer, but also in another diseases including tissue regeneration. PGA has also been used due to its multiva-lency in the development of polymer-based combination therapy applications.

1.3.1 PGA – Poly(glutamic acid) – a Drug carrier with low Polydispersities and Versatile Architectures

NH

O

OO

HN

HN

O

NH

HN

O

O

O- Na+O

Drug

PGA

O- Na+O O- Na+O




Polyglutamates are commonly obtained by ring-opening polymerization (ROP) of amino acid-N-carboxyanhydrides (NCA). The polymerization method enables access to poly-peptidic architectures which are beyond nature’s possibili-ties. Due to the variety of natural and non-natural amino acids and the versatility of the polymerization method a plethora of polypeptides has been created and character-ized, as reviewed in literature. So far, the most promising

chemical approaches are based on initiation of purified NCAs with primary amines, amine hydrochloride salts, heavy metal catalysts or hexamethyldisilazanes. All those methods have certain limitations in the synthesis of well defined polypeptides of high and reproducable quality. The commercial offer so far of PGA was very limited.

In order to overcome these limitations a controlled and living polymerization methodology has been developed based on the modification of the initiators for the ROP of NCAs to produce polypeptides and polypeptide-based block copolymers on a multigram scale. With this con-trolled NCA methodology we managed to enhance the de-gree of polymerization (DP), structural versatility and de-crease polydispersity index (pdi) of polypeptides obtained by NCA polymerization. The method employed effectively suppressed side reactions. Therefore, the control over polymer end groups has been also enhanced enabling the synthesis of well-defined homo or diblock polypeptides of a variety of molecular weight and side-chain and terminal chain functionalities.

# of Monomers n 10 20 50 100 200 300 400 800

Mw (Da) 1.500 3.000 7.500 15.000 30.000 45.000 60.000 120.000

Polydispersity D 1.1~1.2 1.1~1.2 1.1~1.2 1.1~1.2 1.1~1.2 1.1~1.2 1.1~1.2 1.1~1.2

PGA - A Modern versatile Polymer as Drug carrier for Drug Delivery, tissue engineering, Sensing, catalysis, NanoMedicine

Poly(glutamic acid) is a biocompatible and biodegrad-able polymer, which can be conjugated through side chain condensation with any suitable molecule. Due to a controlled proprietary and patented process with living polymerization technology a superior quality of PGA is being achieved. Usual poly amino acids carry significant amounts of cyclic structures, carbamates or isocyanates. Through a very well controlled polymerization process well defined terminal groups and polymeric structures are

being achieved in high purity and with superior polydis-persity. Through “living polymer” technology also multi-functional PGA polymers can be produced through post polymerization modification. PGA can be used for polymer therapeutics application for large biopharmaceuticals and also for small molecule drugs. A controlled loading of small molecules onto PGA polymer can be achieved and brings the advantage of polymer therapy also to small molecules.

HNO

O

O

R

H2N R'

R

H2NNH

O

R'- CO2

HNO

O

O

R

+

HN

NH

HN

NH

R'

O

RO

RO

R

NH

O

O- Na+O

HN

H

ncal

NH

O

O- Na+O

HN

H

ncal

NH

O

O- Na+O

HN

H

ncal

NH

O

O- Na+O

HN

HO

ncal

N33

ncal :_____

10

20

50

100

200

300

400

800




Published Applications:In the following published application PGA equips a hy-drophobic small peptoidic drug molecule, which has poor water solubility with superior pharmacokinetic proper-ties, excellent water solubility, and increased membrane permeability.

Through post polymerization modification PGA can be equipped with additional functional groups, like alkyne or azides for click conjugation; however, also the base polymer can be loaded with different molecules as shown in the following example.

Paclitaxel (PTX) is a widely-used potent cytotoxic drug that also exhibits anti-angiogenic effects at low doses. Its use at its full potential is limited by severe side effects. The PGA polymer PTX nano-scaled conjugate passively targets tumor tissue exploiting enhanced permeability and retention effect. The polymer is enzymatically-degradable leading to PTX release under lysosomal acidic pH. The cy-clic RGD peptide enhances the effect of PGA-PTX alone by targeting ααvβ3

integrin, which is overexpressed on tumor endothelial and epithel cells.

Reference:

f Integrin-assited drug delivery of nano-scaled polymer therapeutics

bearing paclitaxel; Anat Eldar-Boock, Keren Miller, Joaquin Sanchis,

Ruth Lupu, Maria J. Vicent, Ronit Satchi-Fainaro; Biomaterials 2011;

32: 3862-3874.

Reference:

f Modulation of Cellular Apoptosis with Apoptotic Protease-Activation

Factor 1 (Apaf-1) Inhibitors; L. Mondragón, M. Orzáez, G. Sanclimens,

A. Moure, A. Armiñán, P. Sepúlveda, A. Messeguer, M. J. Vicent, E.

Pérez-Payá; J. Med. Chem. 2008; 51: 521-529.

PGA

NH

O

NHO

HN

HN

O

NH

HN

O

O

O- Na+O

PGA - Peptoid Conjugate

O- Na+O O- Na+O

NH

N

O

O

N

O

N

Cl

Cl

O

Cl Cl

O

NH2

NH

O

OO

HN

HN

O

NH

HN

O

O

O- Na+O

Drug

PGA

O- Na+O O- Na+O

PGA

PGA – Peptoid Conjugate

Drug carrier and Release System for Multiple Drug therapy

NH

O

O-Na+O

HN

HN

O

NH

HN

O

O

O-Na+O

O-Na+O O-Na+O




HN

O

nHN

O

m

O

OO

O

HO

O O

O

OH

OO

O HN

O

O

O

HN

O

m-n

OO-Na+

O

HNNH

NHHN

HN

O

O

OO

O

Ph

NH

H2N

HN

OH

O

HN

HN

O

O

NH

NH

HN

HNNHO

O

O

O

O

Ph

HNNH2

NH

HO

O

NH

HN

O

nHN

O

m

O

OO

O

HO

O O

O

OH

OO

O HN

O

O

O

O-Na+O

PGA-PTX-c(RGDfk)2 conjugate

PGA-PTX conjugate

HN

O

n

Na+O-O

PGA

PTX

RGD Peptide

NH

O

OO

HN

NH

HN

O

O

OO

Drug 1 Drug 2

O-Na+O

PGA




Azido: Conjugation via Click Chemistry

Glu: Conjugation via Carbonyl Condensation

Propargyl: Conjugation via Click Chemistry

Glu: Conjugation via Carbonyl Condensation

Bi-functional PGA Drug carrier available for Sophisticated Applications combination therapy – Personalized Medicine

PGA provides ideal possibilities for multi-drug therapies. Already the base PGA polymer can be utilized for these pur-poses, while multifunctional derivatives increase the number of options for the medicinal chemist.

References:

f Canal F, Sanchis J, Vicent MJ.; Polymer-Drug Conjugates as

Nano-Sized Medicines; Current Opin Biotech 2011; doi:10.1016/j.

copbio.2011.06.003.

f Deming, T.; Methodologies for preparation of synthetic block

copolypeptides: Materials with future promise in drug delivery Adv.

Drug Delivery Rev. 2002; 54: 1145-1160.

f Wang, X. Y., Kim, H. J., Wong, C., Vepari, C., Matsumoto, A., Kaplan,

D. L.; Fibrous Proteins – Role in Biomaterials and Tissue Engineer-

ing. Mater. Today 2006; 9: 44-53.

f Dos Santos, S., Chandravarkar, A., Mandal, B., Mimna, R., Murat, K.,

Saucede, L., Tella, P., Tuchscherer, G., Mutter, M.; J. Am. Chem. Soc.

2005; 127: 11888-11889.

f Mart, R. J., Osborne, R. D., Stevens, M. M., Ulijn, R. V.; Peptide-

based stimuli-responsive biomaterials; Soft Matter 2006; 2: 822-835.

f Langer CJ, O’Byrne KJ, Socinski MA, Mikhailov SM, Leniewski-

Kmak K, Smakal M, Ciuleanu TE, Orlov SV, Dediu M, Heigener D,

Eisenfeld AJ, Sandalic L, Oldham FB, Singer JW, Ross HJ; Phase III

trial comparing paclitaxel poliglumex (CTα2103, PPX) in combination

with carboplatin versus standard paclitaxel and carboplatin in the

treatment of PS 2 patients with chemotherapy-naïve advanced nonα

small cell lung cancer; J. Thorac. Oncol. 2008; 3: 623-630.

f Matsumura Y; Poly (amino acid) micelle nanocarriers in preclinical

and clinical studies, Adv. Drug Deliv. Rev.2008; 60: 899-914.

f Matsumura Y, Kataoka K; Preclinical and clinical studies of antican-

cer agentαincorporating polymer micelles, Cancer Sci. 2009: 100: 572-579.

f Cabral H, Matsumoto Y, Mizuno K, Chen Q, Murakami M, Kimura M,

Terada Y, Kano MR, Miyazono K, Uesaka M, Nishiyama N, Kataoka

K.; Nat. Nanotech. 2011; doi:10.1038/nnano.2011.16.

f Marsden HR, Handgraaf JW, Nudelman F, Sommerdijk NA, Kros

A; Uniting polypeptides with sequenceαdesigned peptides: synthesis

and assembly of poly(gammaαbenzyl Lαglutamate)αbαcoiledαcoil

peptide copolymers; J. Am. Chem. Soc. 2010; 132: 2370-2377.

f Zhao C, He P, Xiao C, Gao X, Zhuang X, Chen X.; Synthesis of tem-

perature and pH-responsive crosslinked micelles from polypeptide-

based graft copolymer. J. Colloid. Interface Sci. 2011; 359: 436-442.

f Li C, Wallace S.; Polymer-Drug Conjugates: Recent Development in

Clinical Oncology; Adv. Drug Deliv. Rev. 2008; 60: 886–898.

f Fante C, Eldar-Boock A, Satchi-Fainaro R, Osborn HM, Greco F;

Synthesis and biological evaluation of a polyglutamic acidαdopa-

mine conjugate: a new antiangiogenic agent; J. Med. Chem. 2011; 54: 5255-5259.

f Mondragon L, Orzaez M, Sanclimens G, Moure A, Arminan A, Sepul-

veda P, Messeguer A, Vicent MJ, PerezαPaya E; Modulation of cellular

apoptosis with apoptotic protease-activating factor 1 (Apafα1) inhibi-

tors; J. Med. Chem. 2008; 51: 521-529.

f Fioretti F, Mendoza-Palomares C, Avoaka-Boni MC, Ramaroson J,

Bahi S, Richert L, Granier F, BenkiraneαJessel N, Haikel Y; Nano-

odontology: nanostructured assemblies for endodontic regenera-

tion; J. Biomed. Nanotechnol. 2011; 7: 471-475.

f EldarαBoock A, Miller K, Sanchis J, Lupu R, Vicent MJ, SatchiαFainaro

R; Integrin-assisted drug delivery of nanoαscaled polymer therapeu-

tics bearing paclitaxel; Biomaterials 2011; 32: 3862-3874.

f Leuchs, H. Ber.; Fiber die Glycinαcarbonsäuren; Dtsch. Chem. Ges.

1906; 39: 857.

f Leuchs H, Manasse, W. Ber; Dtsch. Chem. Ges. 1907; 40: 3235.

f Leuchs, H., Geiger, W.; Ber. Dtsch. Chem. Ges. 1908; 41: 1721.

f Deming, T.; Living polymerization of ααamino acidαNαcarboxyanhy-

drides; J. Polym. Sci. 2000; Part A: Polym. Chem. 38: 3011.

f Kricheldorf, H.R.; Polypeptides and 100 Years of Chemistry of α α

Amino Acid NαCarboxyanhydrides; Angew. Chem. Int. Ed. 2006; 45: 5752–5784.

f Hadjichristidis, N., Iatrou, H., Pitsikalis, M., Sakellariou, G.; Synthe-

sis of WellαDefined Polypeptide-Based Materials via the RingαOpen-

ing Polymerization of rαAmino Acid N-Carboxyanhydrides; Chem.

Rev. 2009; 109: 5528–5578.

f Dimitrov I, Schlaad H.; Chem. Comm. 2003; 2944-2945.

f Barz, M., Luxenhofer R., Zentel R., Vicent M.J.; Overcoming the PEG-

addiction: well-defined alternatives to PEG, from structure-property

relationships to better defined therapeutics; Polym. Chem. 2011;

DOI: 10.1039/c0py00406e.

f Vicent MJ, Barz M, Canal F, Conejos I, Duro A; Patent Application n.

P201131713.




PEGs show a spectrum of unique physical and chemical properties, which have been described in literature exten-sively by the pioneers in PEGylation Harris, Veronese and recently by Hermanson. Here are summarized the most common known properties.

f PEG fragments can be attached to many different posi-tions in a protein. Amino groups of any solvent acces-sible lysines as well as the N-terminus are the most prominent candidates for conjugation together with thiol functions of available cysteins. The C-terminus or carboxylic groups from aspartic acid and glutamic acid in theory are also possible for conjugation, how-ever, are rarely used.

f PEG can also serve as spacer or cross linker between two moieties.

f PEG provides high solubility and does not contain charged side chains.

f PEG has been FDA approved for internal application, is non-toxic, lacks T-cell epitopes, and shows no signs of immunogenicity in animal experiments.

f PEG derivatives are available from pure, monodis-perse, discrete molecules with short chain lengths or even one ethylene oxide unit only, to long polydis-perse both linear and branched constructs, allow-ing regio-specific chemical conjugation with small molecules, proteins, peptides and biopharmaceuticals through their broad variety of terminal chemical groups available.

Chemical and Physical Properties of PEGs:

f Good solubility in BOTH hydrophilic AND hydrophobic solvents as: water, toluene, methylene chloride, and many other organic solvents.

f Insoluble in: diethyl ether, hexane, ethylene glycol.

f The solubility is influenced by forming derivatives.

f Highly mobile in water with high exclusion volume; large hydrodynamic radius.

f Form complexes with metal cations.

f Can be used to precipitate proteins and nucleic acids.

f Form two-phase system with aqueous solutions of other polymers.

f Non-toxic, FDA approved for internal consumption.

PEGylating Biopharmaceuticals and Small Mole-cules has the following effects:

f Improves solubility of conjugated molecules.

f Renders proteins non immunogenic and toleragenic.

f Reduces the rate of renal clearance through the kidney and alters pharmacokinetics.

f Renders surface protein rejection.

f Alters electro osmotic flow.

f Moves molecules across cell membranes.

1.3.2 PeG – Poly(ethylene glycol)

Interferon, one of the first PEGylated biopharmaceuticals in the market




References:

f J. Milton Harris (ed.); Poly(Ethylene Glycol) Chemistry Biotechnical

and Biomedical Applications; 1992 Plenum Press, New York; ISBN

0-306-44078-4.

f Veronese, Francesco M., Harris, J. Milton (Editors); Peptide and pro-

tein PEGYlation III: advances in chemistry and clinical applications;

Advanced Drug Delivery Reviews 2008; 60: 1-97.

f Veronese, F. M.; Pasut, G.; “PEGylation, successful approach to drug

delivery”; Drug Discovery Today 2005; 10(21): 1451–1458.

f Veronese, F. M.; Harris, J. M.; “Introduction and overview of peptide

and protein pegylation”, Advanced Drug Delivery Reviews 2002;

54(4): 453–456.

f Greg T. Hermanson; Bioconjugate Techniques; 2008 2nd Edition;

Elsevier; ISBN 978-0-12-370501-3.

f A stepwise Huisegen cycloaddition process: copper (I)-catalyzed

regioselective ligation of azides and terminal alkynes; V.V. Rostovt-

sev, L.G. Green, K.B. Sharpless; Angew. Chem. Int. Ed. 2002; 41: 2596-2599.

f C.W. Tornøe, C. Christensen; M. Meldal; Peptidotriazoles on solid

phase: [1,2,3]-triazoles by regiospecific copper(I)-catalyzed 1,3-dipo-

lar cycloaddition of terminal alkynes to azides; J.Org.Chem. 2002;

67: 3057-3064.

f Click Chemistry: Diverse Chemical Function from a Few Good Reac-

tions; H. C. Kolb, M. G. Finn, and K. Barry

Sharpless, Angew. Chem., Int. Eng. Ed. 2001; 40: 2004-2021.

f The growing impact of click chemistry on drug discovery; H. C. Kolb

and K. Barry Sharpless; Drug Discovery Today 2003; 8(24): 1128-1131.

f Cu-Catalyzed Alkyne-Azide “Click” Cycloadditions from a Mechanis-

tic and Synthetic Perspective; V. C. Bock, H. Hiemstra and J. H. van

Maarseveen; Eur. J. Org. Chem. 2006; 51-68.

f A3-Type Star Polymer via Click Chemistry; O. Altintas, B. Yankul, G.

Hizal and U. Tunca; J. Poly. Sci.: Part A, Polymer Chem. 2006; 44: 6458-6465.

f Preparation of alumina supported copper nanoparticles and their

application in the synthesis of 1,2,3- triazoles; M. L. Kantam, et al.; J.

Mol. Catal. A: Chem. 2006; 256: 273-277.

f A Rapid and Versatile Method to Label Receptor Ligand Using

“Click” Chemistry: Validation with the Muscarinic M1 Antagonist

Pirenzepine; Bioconjugate Chemistry 2006; 17: 1618-1623.

f Alkyne-azide click reaction catalyzed by metallic copper under ul-

trasound; Pedro Cintas1, Alessandro Barge, Silvia Tagliapietra, Luisa

Boffa & Giancarlo Cravotto; Nature Protocols 2010; 5(3): 607-616.

f Davis, F. F.; “The origin of pegnology”; Advanced Drug Delivery

Reviews 2002; 54(4): 457-458.

f Davis, F. F., Van Es, T., and Palczuk, N. C.; 1979; United States Patent

4,179,337.

f Abuchowski, A.; McCoy, J. R.; Palczuk, N. C.; van Es, T. ; Davis, F. F.;

“Effect of covalent attachment of polyethylene glycol on immuno-

genicity and circulating life of bovine liver catalase”; Journal of

Biological Chemistry 1997; 252(11): 3582–3586.

f Fee, C. J.; Van Alstine, J. M.; “PEG-proteins: Reaction engineering

and separation issues”, Chemical Engineering Science 2006; 61(3): 924–939.

f Fee, C. J.; “Protein conjugates purification and characterization”,

PEGylated Protein Drugs: Basic Science and Clinical Applications,

Veronese, F. M., Ed. Birkhauser Publishing: Basel, 2009; 113-125.

f Fee, C. J.; Size-exclusion reaction chromatography (SERC): A new

technique for protein PEGylation; Biotechnology and Bioengineer-

ing 2008; 82(2): 200-206.

f Ryan, S. M.; Giuseppe, M.; Wang, X.; Haddleton, D. M.; Brayden, D.

J.; “Advances in PEGylation of important biotech molecules: delivery

aspects”; Expert Opinion on Drug Delivery 2008; 5(4): 371-383.

f Damodaran V. B.; Fee C. J.; “Protein PEGylation: An overview of

chemistry and process considerations”; European Pharmaceutical

Review 2010; 15(1): 18-26.




The genetic fusion with conformationally disordered polypeptide sequences composed of the amino acids Pro, Ala, and Ser (‘PASylation’) provides a simple way to attach a solvated random chain with large hydrodynamic volume to the protein of biopharmaceutical interest. This amino acid string adopts a bulky random coil structure, which significantly increases the size of the resulting fusion protein, similar to chemical attachment of poly-ethylene glycol (PEG). By this means the typically rapid clearance of the biologically active component via kidney filtration is retarded by 1-2 orders of magnitude. Compared with other strategies to prolong the plasma half-life of biopharmaceu-ticals the PAS-technology possesses several advantages.

Most of the commercially successful first generation bio-pharmaceuticals are small proteins that suffer from rapid renal clearance, leading to disappointingly short circula-tion times. Chemical conjugation of such therapeutic proteins with the random coil polymer PEG to extend their effective size beyond the threshold of kidney filtration has emerged as an established strategy to prolong their plasma half-lives to a clinically useful range.

However, the chemical coupling of a biologically active protein with synthetic polymers has drawbacks with re-spect to biopharmaceutical development and production. Suitable PEG derivatives are expensive, especially as high chemical purity is needed, and their conjugation with a recombinant protein requires additional in vitro process-ing and purification steps, which lower the yield and raise the costs. Furthermore, the pharmaceutical function of a therapeutic protein may be impaired if amino acid side chains in the vicinity of its biochemical active site become chemically modified. Also, PEG is prone to decomposition by oxidation upon storage while, on the other hand, it is not biodegradable, which can cause severe side effects such as vacuolation of organs upon chronic treatment.

PASylation® provides a beneficial solution to these prob-lems on the basis of a «biological» polymer that is solely composed of natural amino acids and protected by a solid IP position.

1.3.3 PASylation technology

Prot

ein

conc

. in

plas

ma

Hydrodynamic volume effect:

DrugPAS 200

PAS 400

Time post i.v. injection

PAS

Therapeutic protein

Expression Vector

Target receptor

Therapeutic protein

PAS

OO

OO

MeO

n

O

N

O

O

NH

HN

NH

OHHN

n

R

O R

O R

O

O

R

H2N

O

R

PEG polymer (activated):

PAS biopolymer:




PASylation® offers several beneficial features, which make this technology attractive for biopharmaceutical drug development:

f PAS sequences adopt a stable random conformation under native buffer conditions and at ambient or body temperature and generate a large hydrodynamic volume, thus increasing the apparent size.

f PASylation® retards renal filtration and, in this way, prolongs plasma half-life of the biological drug by means of a purely biophysical size effect, without any receptor interactions that may influence pharmacody-namics or lead to side effects.

f PAS sequences can be attached via genetic fusion to either the N-terminus, the C-terminus or to both termini of a recombinant protein as well as a spacer between the domains of a bispecific fusion protein.

f PAS sequences can easily be adjusted to pharmaco-logical needs by variation of the polypeptide length.

f PAS sequences are resistant against serum proteases while still being degradable by kidney proteases.

f PAS sequences exhibit high solubility without contain-ing charged side chains.

f PAS sequences do not alter the isoelectric point of the biologically active protein.

f PAS sequences are non-toxic, lack T-cell epitopes, and show no signs of immunogenicity in animal experi-ments.

f PASylation® avoids the need for additional processing and purification steps due to the simple genetic fusion strategy, which allows biotechnological production and recovery together with the therapeutic protein as one single product following established manufactur-ing routes.

f Alternatively, PAS polymers are available as pure (monodisperse) biochemical substances, allowing regio-specific chemical conjugation with proteins, peptides and even small molecule drugs by taking ad-vantage of their singular N-terminal free amino group, among other options.

Improving Biopharmaceuticals by PASylation

PASylation® is a patented technology.

Licenses are available from:

XL-protein GmbH

Lise-Meitner-Str. 30

D-85354 Freising, Germany

Internet: www.xl-protein.com

or through your contact at Iris Biotech GmbH.

PASylating Reagents for chemical conjugation will be available soon through Iris Biotech.




Dendrimers offer a new possibility to derivatize small molecules, surfaces or biopharmaceuticals with a mono-disperse macromolecule and alter in this way properties like solubility and hydrophilicity. Immunogenicity and pharmacokinetics of pharmaceuticals will be improved.

The synthetic approach for designing these dendrons of different generations is based on 2,2-bis(hydroxymethyl) propionic acid, which is a non-toxic and biocompatible building block.

1.3.4 DendrimersApplications with Dendrons

C410

H634

O188

S2, MW = 8635,4 g/mole




The size can be designed from 250 g/mole for 1st genera-tion dendrons to over 4400 g/mole with 5th generation compounds. Dendrimers can be designed reaching even a molecular weight of some 10.000 Da. As focal point alkyne and azido functions are used with appropriate counter parts in any type of click chemistry reaction. Olefinic func-

tions offer the possibility for addition reaction or conjuga-tion by metathesis reactions or photo reactions with the aid of UV light. For the modification of gold surfaces sul-phur bearing dendrons can be used. They also conjugate with biologicals via disulfide bridge formation.

Hydroxyl and acetonide functions are available as termi-nal groups. Thus the surface can be designed as either hydrophilic or hydrophobic. In particular the hydrophobic acetonide variations offer through their amphiphilic nature interesting properties, as the centre is still polar and hydrophilic. This improves solubility in biological liquids. The hydrophobic surface helps to interact with lipids, cell surfaces, and hydrophobic enzymes, like lipases. Furthermore, the acetonides offer another advantages for chemical diversity. They can be removed and thus be a temporary protecting group for further derivatization of the dendritic surface.

References:

f Wu P, Malkoch M, Hunt JN, et al.; Multivalent, bifunctional den-

drimers prepared by click chemistry; Chem. Commun. 2005; 46:

5775-5777. DOI: 10.1039/b512021g

f Antoni P, Malkoch M, Vamvounis G, et al.; Europium confined

cyclen dendrimers with photophysically active triazoles; J. Mater.

Chem. 2008; 18(22): 2545-2554.

f E. R. Gillies and J. M. J. Fréchet, Drug Discovery Today 2005; 10: 35.

f Dual Labeling of Biomolecules by Click Chemistry: a Sequential Ap-

proach. P. Kele, G. Mezö, D. Achatz, O. S. Wolfbeis, Angew. Chem.

2009; 121: 350-353; Angew. Chem. Intl. Ed. 2009; 48: 344-347. DOI:

10.1002/ange.200804514.




Possible Applications of Dendrons f Interesting versatile building block for further chemi-

cal derivatization;

f Improve drug delivery and pharmacokinetics of small molecules and biopharmaceuticals;

f Functionalization of surfaces;

f Conjugation with biopharmaceuticals, antibodies and other biologicals via disulfide bridge;

f Coupling with proteins to improve their stability towards immunogenic degradation;

f Altering enzymes to increase their chemical resistance and thermostability;

f Conjugation with dyes, fluorescence labels, spin mark-ers and other chemical probes.

On stock available: azido, alkyne, allyl, disulfide

Conjugation with On custom basis available: Male-inimides, biotinyl, NHS esters

Conjugation with

Alkynes via

Click reaction

Azides via

Click reaction

Olefines via metathesis Other partners with UV

Gold surfaces

SH from proteins

N

O

O

O

O

N

O

O

O

S

NH

NH

O

SH from proteins

Streptavidin

NH2 from Proteins, dyes, probes and other reaction partners

On stock available:With Azido, Alkyne, Allyl and Disulfide function at the fo-cal point there are four functional groups available, which

offer a wide variety of reactions.

On custom basis:Maleinimides, Biotinyl and NHS esters are available op-tions, which can be supplied on request.

Please inquire for any other Option or Larger Quantities!

Properties of Dendrons f Monodisperse macromolecules from 250 g/mole to

4400 g/mole;

f The dendron surface can be amphiphilic, hydrophilic or hydrophobic;

f Easy post modification;

f Different anchoring possibilities through a variety of available chemical functions of the focal point;




PGA1005 nBu-PGA(20)[Na]PGA1005.0500 500 mg € 425,00

PGA1005.0001 1 g € 575,00

PGA1005.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

20

n-Butyl-poly(L-glutamic acid) sodium salt (MW 3000Da) MOLECULAR WEIGHT: 3000 Da


PGA1015.0001 1 g € 575,00

PGA1015.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

100



PGA1025.0001 1 g € 575,00

PGA1025.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

300



PGA1030.0001 1 g € 575,00

PGA1030.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

400



PGA1000.0001 1 g € 575,00

PGA1000.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

10



PGA1010.0001 1 g € 575,00

PGA1010.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

50



PGA1020.0001 1 g € 575,00

PGA1020.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

200


2. Available PGA - Poly(glutamic acid) DerivativesProduced by patent controlled process delivering high quality carriers, suitable for pharma applications.

2.1 Poly(glutamic acid) Base Polymers2.1.1 Alkyl terminated PGA

Article No. Quantity Price


PGA1035.0001 1 g € 575,00

PGA1035.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

800





PGA1040 Npt-PGA(10)[Na]PGA1040.0500 500 mg € 425,00

PGA1040.0001 1 g € 575,00

PGA1040.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

10

neo-Pentyl-poly(L-glutamic acid) sodium salt (MW 1500Da) MOLECULAR WEIGHT: 1500 Da


PGA1050.0001 1 g € 575,00

PGA1050.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

50



PGA1060.0001 1 g € 575,00

PGA1060.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

200



PGA1070.0001 1 g € 575,00

PGA1070.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

400



PGA1045.0001 1 g € 575,00

PGA1045.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

20



PGA1055.0001 1 g € 575,00

PGA1055.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

100



PGA1065.0001 1 g € 575,00

PGA1065.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

300



PGA1075.0001 1 g € 575,00

PGA1075.0005 5 g € 2250,00

NH

(S)(S)HN

H

O- Na+O

O

800






PGA1085 Prg-PGA(20)[Na]PGA1085.0500 500 mg € 550,00

PGA1085.0001 1 g € 825,00

PGA1085.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

20

Propargyl-poly(L-glutamic acid) sodium salt (MW 3000Da) MOLECULAR WEIGHT: 3000 Da


PGA1095.0001 1 g € 825,00

PGA1095.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

100



PGA1105.0001 1 g € 825,00

PGA1105.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

300



PGA1115.0001 1 g € 825,00

PGA1115.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

800



PGA1080.0001 1 g € 825,00

PGA1080.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

10



PGA1090.0001 1 g € 825,00

PGA1090.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

50



PGA1100.0001 1 g € 825,00

PGA1100.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

200



PGA1110.0001 1 g € 825,00

PGA1110.0005 5 g € 2450,00

NH

(S)(S)HN

H

O- Na+O

O

400


2.1.2 click terminated PGA Article No. Quantity Price

Superior PGA Quality by controlled ROP production technology – ideal for pharma applications.




PGA1120 N3-PGA(10)[Na]PGA1120.0500 500 mg € 600,00

PGA1120.0001 1 g € 900,00

PGA1120.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

10

ON3 3

Azido-ethyltri(ethylene glycol)-poly(L-glutamic acid) sodium salt (MW 1500Da) MOLECULAR WEIGHT: 1500 Da

PGA1125 N3-PGA(20)[Na]PGA1125.0500 500 mg € 600,00

PGA1125.0001 1 g € 900,00

PGA1125.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

20

ON3 3


PGA1135 N3-PGA(100)[Na]PGA1135.0500 500 mg € 600,00

PGA1135.0001 1 g € 900,00

PGA1135.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

100

ON3 3


PGA1145 N3-PGA(300)[Na]PGA1145.0500 500 mg € 600,00

PGA1145.0001 1 g € 900,00

PGA1145.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

300

ON3 3


PGA1155 N3-PGA(800)[Na]PGA1155.0500 500 mg € 600,00

PGA1155.0001 1 g € 900,00

PGA1155.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

800

ON3 3


PGA1130 N3-PGA(50)[Na]PGA1130.0500 500 mg € 600,00

PGA1130.0001 1 g € 900,00

PGA1130.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

50

ON3 3


PGA1140 N3-PGA(200)[Na]PGA1140.0500 500 mg € 600,00

PGA1140.0001 1 g € 900,00

PGA1140.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

200

ON3 3


PGA1150 N3-PGA(400)[Na]PGA1150.0500 500 mg € 600,00

PGA1150.0001 1 g € 900,00

PGA1150.0005 5 g € 2750,00

NH

(S)(S)HN

H

O- Na+O

O

400

ON3 3


Inquire for any different terminal group or molecular weight.





PGA1180 nBu-PGA(200)[Prg(10)] PGA1180.0100 100 mg € 400,00

PGA1180.0500 5 g € 725,00

PGA1180.0001 1 g € 1100,00

PGA1180.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

n-Butyl-poly(L-glutamic acid gamma-propargyl amide) sodium salt (5-10 mol% propargyl substitution, MW 30000Da) MOLECULAR WEIGHT: 30000 Da

PGA1190 nBu-PGA(20)[Prg(20)]PGA1190.0100 100 mg € 425,00

PGA1190.0500 500 mg € 775,00

PGA1190.0001 1 g € 1175,00

PGA1190.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x



PGA1175.0500 500 mg € 725,00

PGA1175.0001 1 g € 1100,00

PGA1175.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x



PGA1185.0500 500 mg € 775,00

PGA1185.0001 1 g € 1175,00

PGA1185.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x



PGA1165.0500 500 mg € 725,00

PGA1165.0001 1 g € 1100,00

PGA1165.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x



PGA1170.0500 500 mg € 725,00

PGA1170.0001 1 g € 1100,00

PGA1170.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x



PGA1160.0500 500 mg € 725,00

PGA1160.0001 1 g € 1100,00

PGA1160.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x


2.2 Poly(glutamic acid) copolymers2.2.1 Alkyl terminated click-PGA copolymer

By controlled living polimerization methodology

dedicated block copolymers can be designed.






PGA1200.0500 500 mg € 775,00

PGA1200.0001 1 g € 1175,00

PGA1200.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x


PGA1210 Npt-PGA(10)[Prg(10)] PGA1210.0100 100 mg € 400,00

PGA1210.0500 500 mg € 725,00

PGA1210.0001 1 g € 1100,00

PGA1210.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

neo-Pentyl-poly(L-glutamic acid gamma-propargyl amide) sodium salt (5-10 mol% propargyl substitution, MW 1500Da) MOLECULAR WEIGHT: 1500 Da


PGA1215.0500 500 mg € 725,00

PGA1215.0001 1 g € 1100,00

PGA1215.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x



PGA1220.0500 500 mg € 725,00

PGA1220.0001 1 g € 1100,00

PGA1220.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x



PGA1195.0500 500 mg € 775,00

PGA1195.0001 1 g € 1175,00

PGA1195.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x



PGA1205.0500 500 mg € 775,00

PGA1205.0001 1 g € 1175,00

PGA1205.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x





We offer 10 and 20 % of copolymer – inquire for your requirement.


PGA1230.0500 500 mg € 725,00

PGA1230.0001 1 g € 1100,00

PGA1230.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x



PGA1225.0500 500 mg € 725,00

PGA1225.0001 1 g € 1100,00

PGA1225.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x






PGA1240.0500 500 mg € 775,00

PGA1240.0001 1 g € 1175,00

PGA1240.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x



PGA1250.0500 500 mg € 775,00

PGA1250.0001 1 g € 1175,00

PGA1250.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x


PGA1260 nBu-PGA(10)[PEG2-N3(10)] PGA1260.0100 100 mg € 575,00

PGA1260.0500 500 mg € 860,00

PGA1260.0001 1 g € 1300,00

PGA1260.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

3

n-Butyl-poly(L-glutamic acid gamma-azido-ethyltri(ethylene glycol) amide) sodium salt (5-10 mol% azido substitution, MW 1600Da) MOLECULAR WEIGHT: 1600 Da


PGA1265.0500 500 mg € 860,00

PGA1265.0001 1 g € 1300,00

PGA1265.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

3



PGA1270.0500 500 mg € 860,00

PGA1270.0001 1 g € 1300,00

PGA1270.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

3



PGA1235.0500 500 mg € 775,00

PGA1235.0001 1 g € 1175,00

PGA1235.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x



PGA1245.0500 500 mg € 775,00

PGA1245.0001 1 g € 1175,00

PGA1245.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x



PGA1255.0500 500 mg € 775,00

PGA1255.0001 1 g € 1175,00

PGA1255.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x






PGA1275.0500 500 mg € 860,00

PGA1275.0001 1 g € 1300,00

PGA1275.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

3






PGA1190.0500 500 mg € 775,00

PGA1190.0001 1 g € 1175,00

PGA1190.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x



PGA1200.0500 500 mg € 775,00

PGA1200.0001 1 g € 1175,00

PGA1200.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x



PGA1210.0500 500 mg € 725,00

PGA1210.0001 1 g € 1100,00

PGA1210.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x



PGA1215.0500 500 mg € 725,00

PGA1215.0001 1 g € 1100,00

PGA1215.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x



PGA1185.0500 500 mg € 775,00

PGA1185.0001 1 g € 1175,00

PGA1185.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x



PGA1195.0500 500 mg € 775,00

PGA1195.0001 1 g € 1175,00

PGA1195.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x



PGA1205.0500 500 mg € 775,00

PGA1205.0001 1 g € 1175,00

PGA1205.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x



PGA Copolymer with reactive side chains for Click Conjugation.

Superior PGA quality through controlled ROP technology.


PGA1280.0500 500 mg € 860,00

PGA1280.0001 1 g € 1300,00

PGA1280.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

3






PGA1230.0500 500 mg € 725,00

PGA1230.0001 1 g € 1100,00

PGA1230.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x



PGA1240.0500 500 mg € 775,00

PGA1240.0001 1 g € 1175,00

PGA1240.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x



PGA1250.0500 500 mg € 775,00

PGA1250.0001 1 g € 1175,00

PGA1250.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x



PGA1260.0500 500 mg € 860,00

PGA1260.0001 1 g € 1300,00

PGA1260.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

3



PGA1265.0500 500 mg € 860,00

PGA1265.0001 1 g € 1300,00

PGA1265.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

3



PGA1225.0500 500 mg € 725,00

PGA1225.0001 1 g € 1100,00

PGA1225.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x



PGA1235.0500 500 mg € 775,00

PGA1235.0001 1 g € 1175,00

PGA1235.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x



PGA1245.0500 500 mg € 775,00

PGA1245.0001 1 g € 1175,00

PGA1245.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x



PGA1255.0500 500 mg € 775,00

PGA1255.0001 1 g € 1175,00

PGA1255.0005 5 g € 3400,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x




PGA1220.0500 500 mg € 725,00

PGA1220.0001 1 g € 1100,00

PGA1220.0005 5 g € 3250,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x






PGA1270.0500 500 mg € 860,00

PGA1270.0001 1 g € 1300,00

PGA1270.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

3



PGA1275.0500 500 mg € 860,00

PGA1275.0001 1 g € 1300,00

PGA1275.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

3



PGA1280.0500 500 mg € 860,00

PGA1280.0001 1 g € 1300,00

PGA1280.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

3



PGA1285.0500 500 mg € 1000,00

PGA1285.0001 1 g € 1450,00

PGA1285.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

3



PGA1290.0500 500 mg € 1000,00

PGA1290.0001 1 g € 1450,00

PGA1290.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

3



PGA1295.0500 500 mg € 1000,00

PGA1295.0001 1 g € 1450,00

PGA1295.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

3



PGA1300.0500 500 mg € 1000,00

PGA1300.0001 1 g € 1450,00

PGA1300.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

3



PGA1305.0500 500 mg € 1000,00

PGA1305.0001 1 g € 1450,00

PGA1305.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

3





We offer 10 and 20 % of copolymer – inquire for your requirement.




PGA1310 Npt-PGA(10)[PEG2-N3(10)] PGA1310.0100 100 mg € 575,00

PGA1310.0500 500 mg € 860,00

PGA1310.0001 1 g € 1300,00

PGA1310.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

3

neo-Pentyl-poly(L-glutamic acid gamma-azido-ethyltri(ethylene glycol) amide) sodium salt (5-10 mol% azido substitution, MW 1600Da) MOLECULAR WEIGHT: 1600 Da


PGA1315.0500 500 mg € 860,00

PGA1315.0001 1 g € 1300,00

PGA1315.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

3



PGA1320.0500 500 mg € 860,00

PGA1320.0001 1 g € 1300,00

PGA1320.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

3



PGA1325.0500 500 mg € 860,00

PGA1325.0001 1 g € 1300,00

PGA1325.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

3



PGA1330.0500 500 mg € 860,00

PGA1330.0001 1 g € 1300,00

PGA1330.0005 5 g € 4575,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

3



PGA1335.0500 500 mg € 1000,00

PGA1335.0001 1 g € 1450,00

PGA1335.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

3



PGA1340.0500 500 mg € 1000,00

PGA1340.0001 1 g € 1450,00

PGA1340.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

3



PGA1345.0500 500 mg € 1000,00

PGA1345.0001 1 g € 1450,00

PGA1345.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

3



PGA1350.0500 500 mg € 1000,00

PGA1350.0001 1 g € 1450,00

PGA1350.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

3



PGA1355.0500 500 mg € 1000,00

PGA1355.0001 1 g € 1450,00

PGA1355.0005 5 g € 4850,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

3







PGA1360.0500 500 mg € 2575,00

PGA1360.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

7

n-Butyl-poly(L-glutamic acid gamma-azido-ethylhepta(ethylene glycol) amide) sodium salt (5-10 mol% azido substitution, MW 1800Da) MOLECULAR WEIGHT: 1800 Da


PGA1365.0500 500 mg € 2575,00

PGA1365.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

7



PGA1370.0500 5 g € 2575,00

PGA1370.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

7



PGA1375.0500 500 mg € 2575,00

PGA1375.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

7



PGA1380.0500 500 mg € 2575,00

PGA1380.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

7



PGA1385.0500 500 mg € 3000,00

PGA1385.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

7



PGA1390.0500 500 mg € 3000,00

PGA1390.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

7



PGA1395.0500 500 mg € 3000,00

PGA1395.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

7



PGA1400.0500 500 mg € 3000,00

PGA1400.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

7



PGA1405.0500 500 mg € 3000,00

PGA1405.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

7







PGA1410.0500 500 mg € 2575,00

PGA1410.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

7

neo-Pentyl-poly(L-glutamic acid gamma-azido-ethylhepta(ethylene glycol) amide) sodium salt (5-10 mol% azido substitution, MW 1800Da) MOLECULAR WEIGHT: 1800 Da


PGA1415.0500 500 mg € 2575,00

PGA1415.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

7

neo-Pentyl-poly(L-glutamic acid gamma-azido-ethylhepta(ethylene gly-col) amide) sodium salt (5-10 mol% azido substitution, MW 3600Da) MOLECULAR WEIGHT: 3600 Da


PGA1420.0500 500 mg € 2575,00

PGA1420.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

7



PGA1425.0500 500 mg € 2575,00

PGA1425.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

7



PGA1430.0500 500 mg € 2575,00

PGA1430.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

7



PGA1435.0500 500 mg € 3000,00

PGA1435.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

ON3

7



PGA1440.0500 500 mg € 3000,00

PGA1440.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

ON3

7



PGA1445.0500 500 mg € 3000,00

PGA1445.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

ON3

7



PGA1450.0500 500 mg € 3000,00

PGA1450.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

ON3

7



PGA1455.0500 500 mg € 3000,00

PGA1455.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

ON3

7






2.2.2 Alkyl terminated mPeG-PGA co-PolymerPGA1460 nBu-PGA(10)[mPEG(10)] PGA1460.0100 100 mg € 860,00

PGA1460.0500 500 mg € 2575,00

PGA1460.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6

n-Butyl-poly(L-glutamic acid gamma-(omega-methoxyhepta(ethylene glycol))) sodium salt (5-10 mol% mPEG substitution, MW 1800Da) MOLECULAR WEIGHT: 1800 Da

PGA1465 nBu-PGA(20)[mPEG(10)] PGA1465.0100 100 mg € 860,00

PGA1465.0500 500 mg € 2575,00

PGA1465.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6



PGA1470.0500 500 mg € 2575,00

PGA1470.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6



PGA1475.0500 500 mg € 2575,00

PGA1475.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6



PGA1480.0500 500 mg € 2575,00

PGA1480.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6



PGA1485.0500 500 mg € 3000,00

PGA1485.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6



PGA1490.0500 500 mg € 3000,00

PGA1490.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6



PGA1495.0500 500 mg € 3000,00

PGA1495.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6



PGA copolymer with mPEG to reduce charge induced interactions.

PGA - mPEG copolymers for improved blood circulation.





PGA1500.0500 500 mg € 3000,00

PGA1500.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6



PGA1505.0500 500 mg € 3000,00

PGA1505.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6


PGA1510 Npt-PGA(10)[mPEG(10)] PGA1510.0100 100 mg € 860,00

PGA1510.0500 500 mg € 2575,00

PGA1510.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6

neo-Pentyl-poly(L-glutamic acid gamma-(omega-methoxyhepta(ethylene glycol))) sodium salt (5-10 mol% mPEG substitution, MW 1800Da) MOLECULAR WEIGHT: 1800 Da


PGA1515.0500 500 mg € 2575,00

PGA1515.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6



PGA1520.0500 500 mg € 2575,00

PGA1520.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6



PGA1525.0500 500 mg € 2575,00

PGA1525.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6



PGA1530.0500 500 mg € 2575,00

PGA1530.0001 1 g € 3875,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6



PGA1535.0500 500 mg € 3000,00

PGA1535.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6



PGA1540.0500 500 mg € 3000,00

PGA1540.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6



PGA1545.0500 500 mg € 3000,00

PGA1545.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6







PGA1550.0500 500 mg € 3000,00

PGA1550.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6



PGA1555.0500 500 mg € 3000,00

PGA1555.0001 1 g € 4500,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6


2.2.3 click terminated mPeG-PGA co-PolymerPGA1560 Prg-PGA(10)[mPEG(10)] PGA1560.0100 100 mg € 890,00

PGA1560.0500 500 mg € 2660,00

PGA1560.0001 1 g € 3990,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6

Propargyl-poly(L-glutamic acid gamma-(omega-methoxyhepta(ethylene glycol))) sodium salt (5-10 mol% mPEG substitution, MW 1800Da) MOLECULAR WEIGHT: 1800 Da

PGA1565 Prg-PGA(20)[mPEG(10)] PGA1565.0100 100 mg € 890,00

PGA1565.0500 500 mg € 2660,00

PGA1565.0001 1 g € 3990,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6



PGA1570.0500 500 mg € 2660,00

PGA1570.0001 1 g € 3990,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6



PGA1575.0500 500 mg € 2660,00

PGA1575.0001 1 g € 3990,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6



PGA1580.0500 500 mg € 2660,00

PGA1580.0001 1 g € 3990,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6



PGA copolymer with mPEG to reduce charge induced interactions.

PGA - mPEG copolymers for improved blood circulation.

With Click Terminus for sophisticated applications in diagnostics.





PGA1585.0500 500 mg € 3100,00

PGA1585.0001 1 g € 4650,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6



PGA1590.0500 500 mg € 3100,00

PGA1590.0001 1 g € 4650,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6



PGA1595.0500 500 mg € 3100,00

PGA1595.0001 1 g € 4650,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6



PGA1600.0500 500 mg € 3100,00

PGA1600.0001 1 g € 4650,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6



PGA1605.0500 500 mg € 3100,00

PGA1605.0001 1 g € 4650,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6



N

SHO

S

(S)(S)N

O

OH

RS

(S)(S)N

O-AMP

O

-PPi

+ ATP

RS

N

O-AMP

O

- H+

RS

N

O-AMP

O

+O2

OO- AMPR

S

N

O

OO

- CO2

N

SHO

S

N O

N

SHO

S

(S)(S)N

O

OH

RS

(S)(S)N

O-AMP

O

-PPi

+ ATP

RS

N

O-AMP

O

- H+

RS

N

O-AMP

O

+O2

OO- AMPR

S

N

O

OO

- CO2

N

SHO

S

N O

N

SHO

S

N O

Luciferin – enzyme Substate for Life Sciences Applications

Interested in more Enzyme Substrates – visit our website www.iris-biotech.de

In nature, the American firefly (photinus pyralis) uses the luciferase bioluminescence to find a partner for reproduc-tion. The result of the luciferase reaction is the emission of yellow-green light at 560 nm. This reaction requires the enzyme luciferase, the substrate D-Luciferin and the co-factors ATP, Mg2+ and Oxygen. The reaction is a cascade of several steps: the initial adenylation of Luciferin is follo-

wed by oxidation to Oxyluciferin.

The Oxyluciferin resulting from this reaction is in an electronically excited state. On relaxation to ground state a photon is released (from 550 nm (yellow-green) at neutral pH to 620 nm (red) at low pH).




PGA1610 N3-PGA(10)[mPEG(10)] PGA1610.0100 100 mg € 930,00

PGA1610.0500 500 mg € 2790,00

PGA1610.0001 1 g € 4180,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6

ON3

3

Azido-ethyltri(ethylene glycol)-poly(L-glutamic acid gamma-(omega-methoxyhepta(ethylene glycol))) sodium salt (5-10 mol% mPEG substitution, MW 1800Da) MOLECULAR WEIGHT: 1800 Da


PGA1615.0500 500 mg € 2790,00

PGA1615.0001 1 g € 4180,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6

ON3

3



PGA1620.0500 500 mg € 2790,00

PGA1620.0001 1 g € 4180,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6

ON3

3



PGA1625.0500 500 mg € 2790,00

PGA1625.0001 1 g € 4180,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6

ON3

3

Azido-ethyltri(ethylene glycol)-poly(L-glutamic acid gamma-(omega-methoxyhepta(ethylene glycol))) sodium salt (5-10 mol% mPEG substi-tution, MW 18400Da) MOLECULAR WEIGHT: 18400 Da


PGA1630.0500 500 mg € 2790,00

PGA1630.0001 1 g € 4180,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6

ON3

3

Azido-ethyltri(ethylene glycol)-poly(L-glutamic acid gamma-(omega-methoxyhepta(ethylene glycol))) sodium salt (5-10 mol% mPEG substi-tution, MW 36900Da) MOLECULAR WEIGHT: 36900 Da


PGA1635.0500 500 mg € 3225,00

PGA1635.0001 1 g € 4825,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

10 - x

OOMe

6

ON3

3



PGA1640.0500 500 mg € 3225,00

PGA1640.0001 1 g € 4825,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

20 - x

OOMe

6

ON3

3



PGA1645.0500 500 mg € 3225,00

PGA1645.0001 1 g € 4825,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

50 - x

OOMe

6

ON3

3



PGA1650.0500 500 mg € 3225,00

PGA1650.0001 1 g € 4825,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

100 - x

OOMe

6

ON3

3



PGA1655.0500 500 mg € 3225,00

PGA1655.0001 1 g € 4825,00

NH

(S)(S)HN

NH

O

x

(S)(S) NH

H

O

O O- Na+

O

200 - x

OOMe

6

ON3

3






Impart significant water solubility; the PEGylation reagent itself is non-immunogenic and non-toxic, passing these properties to the PEGylated biopharmaceutical.

Potentially very useful as a drug/protein modifier to spe-cifically increase hydrodynamic volume.

Produces compounds with reduced aggregation, or surfaces with reduced non-specific binding in diagnostic applications.

Branched PEGs are highly methylene chloride soluble, the ideal solvent for carboamide activations.

Reference:

Greg T. Hermanson, Bioconjugate Techniques, 2nd Ed, Elsevier Inc.,

Burlington, MA 01803, April, 2008 (ISBN-13: 978-0-12-370501-3; ISBN-10:

0-12-370501-0)., Ch. 18, pp. 711-742.

3. Available monodisperse, polydisperse and branched PeGylating Reagents


PEG0173 H2N-[mPEG(4)]4 PEG0173.0100 100 mg € 180,00

PEG0173.0500 500 mg € 710,00O

O

OHN O

OO

ONO

OO

ONH

O

ONH

O

OO

ONO

OO

OHNO

NH2

2-amino-N1,N

5-bis(15,20-dioxo-2,5,8,11-tetraoxa-14,19-diaza-

henicosan-21-yl)-N1,N

5-di(2,5,8,11-tetraoxatridecan-13-yl)pentanediamide

CAS-NO: FORMULA: C53

H103

N7O

22

MOLECULAR WEIGHT: 1190,42 g/mole

PEG0216 H2N-[mPEG(4)-mPEG(10)]2 PEG0216.0100 100 mg € 300,00

PEG0216.0500 500 mg € 1180,00O

O

OHN O

MeO

ON

OO

ONH

OMe

ONH

O

MeO

ON

OO

OHNO

Me

NH2

10

10

2-amino-N1,N

5-bis(15,20-dioxo-2,5,8,11-tetraoxa-14,19-diaza-

henicosan-21-yl)-N1,N

5-bis[omega-methoxy-undeca(ethylenglycol)-

omega-yl]pentanediamide CAS-NO: FORMULA: C

81H

159N

7O

36


PEG2295 H2N-mPEG(4)-[mPEG(4)]3 PEG2295.0100 100 mg € 375,00

PEG2295.0001 1 g € 1200,00

OOOOH2N

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me3

3

3

Amino-PEG(4)-[PEG(4)-OMe]3 CAS-NO: FORMULA: C

51H

101N

5O

23

MOLECULAR WEIGHT: 1152,37 g/moleFURTHER INFORMATION: spacer is 37 atoms and 21 A

PEG2315 H2N-PEG(4)-[mPEG(8)]3 PEG2315.0100 100 mg € 375,00

PEG2315.0001 1 g € 1200,00

OOOOH2N

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me7

7

7


75H

149N

5O

35

MOLECULAR WEIGHT: 1681 g/moleFURTHER INFORMATION: spacer is 49 atoms and 50 A

PEG1325 H2N-dPEG™(4)-[mPEG(12)]3 PEG1325.0100 100 mg € 375,00

PEG1325.0001 1 g € 1200,00

OOOOH2N

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me11

11

11


99H

197N

5O

47

MOLECULAR WEIGHT: 2209,63 g/moleFURTHER INFORMATION: spacers are 61 atoms and 63

PEG3350 H2N-PEG(4)-[mdPEG™(24)]3 PEG3350.0100 100 mg € 425,00

PEG3350.1000 1 g € 1600,00

OOOOH2N

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me23

23

23


171H

341N

5O

83

MOLECULAR WEIGHT: 3795,52 g/moleFURTHER INFORMATION: Spacer length 97 atoms or 96.2 A

3.1 Branched PeGylating Reagents




PEG4640 Aminoxy-dPEG™(12+12)-[mdPEG™(11)]3 PEG4640.0100 100 mg € 550,00

PEG4640.1000 1 g € 2200,00

12

H2NO

OHN

O

O NH

OO

OHN

O

O

HN

O

O NH

O

O

O

12

11

11

11

alpha-Aminoxy-bis[dodeca(ethylene glycol)]-tris(omega-methoxy-undeca(ethylene glycol)] CAS-NO: FORMULA: C

136H

270N

6O

66

MOLECULAR WEIGHT: 3045,60 g/moleFURTHER INFORMATION: -

PEG2305 HOOC-PEG(4)-[mPEG(4)]3 PEG2305.0100 100 mg € 375,00

PEG2305.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me3

3

3

HO

OO

Carboxy-PEG(4)-[PEG(4)-OMe]3 CAS-NO: FORMULA: C

56H

107N

5O

26



PEG2325.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me7

7

7

HO

OO

Carboxy-PEG(4)-[PEG(8)-OMe]3 CAS-NO: FORMULA: C

80H

155N

5O

38

MOLECULAR WEIGHT: 1795,1 g/moleFURTHER INFORMATION: spacer is 55 atoms and 60.2 A


PEG1490.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me11

11

11

HO

OO

Carboxy-PEG(4)-[PEG(12)-OMe]3 Tris((37-N-amido-2,5,8,11,14,17,20,23,26,29,32,35-dodecaoxa-heptatriacontane)-4-oxapentanoyl)-15-(N-glutaroylamido)-4,7,10,13-tetraoxapentadecanoylamido)methane CAS-NO: FORMULA: C

104H

203N

5O

50



PEG3240.1000 1 g € 1600,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me23

23

23

HO

OO

Carboxyl-PEG(4)-[PEG(24)-OMe]3 CAS-NO: FORMULA: C

176H

347N

5O

86


Aldehydes are common in carbohydrates, carbohydrate containing proteins, oxidizable matrices, among others

and also can be incorporated using appropriate reagents, like glucar dialdehyde or more sophisticated derivatives.


H2NO

O

H NO

H

+

PEG

PEGPE

GPEG

PEG

PEG




PEG0183 NHS-[mPEG(4)]4 PEG0183.0100 100 mg € 210,00

PEG0183.0500 500 mg € 830,00

O

O

N

O

O

OHN O

OO

ONO

OO

ONH

O

ONH

O

OO

ONO

OO

OHNO

NH

O O

O

2,5-dioxopyrrolidin-1-yl 26-((15,20-dioxo-2,5,8,11-tetraoxa-14,19-diaza-henicosan-21-yl)(2,5,8,11-tetraoxatridecan-13-yl)carbamoyl)-15,20,23,28-tetraoxo-22-(2,5,8,11-tetraoxatridecan-13-yl)-2,5,8,11-tetraoxa-14,19,22,27-tetraazadotriacontan-32-oate CAS-NO: FORMULA: C

62H

112N

8O

27


PEG2060 6-arm-mPEG-NHS PEG2060.0000 Please inquire!

OHN

NH

O

N

O

OO

O

OS

O

HN

O

O

S

S

NH

O

NH

O

NH

O

ONH

ONH

ONH

NH

O

NH

O

OO

OO

OO

OO

OO

OO

10

10

10

10

10

10

Hexakis(undeka(ethylene glycol))-succinimidyl ester CAS-NO: FORMULA: C

187H

358N

12O

84S

3


PEG2300 NHS-PEG(4)-[mPEG(4)]3 PEG2300.0100 100 mg € 375,00

PEG2300.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me3

3

3

O

OON

O

O

Succinimidyl-PEG(4)-[PEG(4)-OMe]3 CAS-NO: FORMULA: C

60H

110N

6O

28



PEG2320.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me7

7

7

O

OON

O

O


84H

158N

6O

40


PEG1840 NHS-dPEG™(4)-[mPEG(12)]3 PEG1840.0100 100 mg € 375,00

PEG1840.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me11

11

11

O

OON

O

O

Succinimidyl-PEG(4)-[PEG(12)-OMe]3 Tris((37-N-amido-2,5,8,11,14,17,20,23,26,29,32,35-dodecaoxa-heptatriacontane)-4-oxapentanoyl)-15-(N-glutaroylamido)-4,7,10,13-tetraoxapentadecanoylamido)methane N-hydroxysuccinimidyl ester CAS-NO: FORMULA: C

108H

206N

6O

52



PEG3230.1000 1 g € 1600,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me23

23

23

O

OON

O

O


180H

350N

6O

88

MOLECULAR WEIGHT: 4006,69 g/moleFURTHER INFORMATION: Spacer is 103 atoms or 107.1 A

PEG2310 mal-PEG(4)-[mPEG(4)]3 PEG2310.0100 100 mg € 375,00

PEG2310.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me3

3

3

N

OO

O

Maleinimido-PEG(4)-[PEG(4)-OMe]3 CAS-NO: FORMULA: C

58H

106N

6O

26







PEG2340.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me7

7

7

N

OO

O

Maleinimido-PEG(4)-[PEG(8)-OMe]3 CAS-NO: FORMULA: C

82H

154N

6O

38



PEG1610.0001 1 g € 1200,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me11

11

11

N

OO

O

Maleinimido-PEG(4)-[PEG(12)-OMe]3 ester CAS-NO: FORMULA: C

106H

202N

6O

50



PEG3420.1000 1 g € 1600,00

OOOONH

O

NH

O

O

O NH

O O MeO

O

HN

OHN

O O Me

O O Me23

23

23

N

OO

O

Maleinimido-PEG(4)-[PEG(24)-OMe]3 ester CAS-NO: FORMULA: C

178H

346N

6O

86

MOLECULAR WEIGHT: 3946.64 g/moleFURTHER INFORMATION: Spacer is 103 atoms or 108.3 A

PEG1480 Bis-mal-Oc-NH2*TFA PEG1480.0100 100 mg € 350,00

PEG1480.0001 1 g € 930,00

N NH

HN

O

O

O

O

NH2

NHO

N OO

N,N‘-(6-(6-aminohexylamino)-6-oxohexane-1,5-diyl)bis(3-maleinimido-propanamide) CAS-NO: FORMULA: C

26H

38N

6O

7*CF

3CO

2H

MOLECULAR WEIGHT: 546,62*114,02 g/moleFURTHER INFORMATION: Spacer are 17 and 21 atoms and 19.1 and 19.6 A

PeG-fatty acid derivatives, which are water soluble adjuvants.PEG0306 Palm3-Cys-PEG-OH PEG0306.0005 5 mg € 100,00

PEG0306.0025 25 mg € 250,00

PEG0306.0100 100 mg € 400,00O

O

O

S

O

NH

OO NH

OOH

nalpha-[(O,O‘-N-Trispalmitoyl)-2-amino-5,6-dihydroxy-4-thia-hexanoylamido]-omega-hydroxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -

PEG0506 Palm3-Cys-PEG-OH PEG0506.0005 5 mg € 100,00

PEG0506.0025 25 mg € 250,00

PEG0506.0100 100 mg € 400,00O

O

O

S

O

NH

OO NH

OOH

nalpha-[(O,O‘-N-Trispalmitoyl)-2-amino-5,6-dihydroxy-4-thia-hexanoylamido]-omega-hydroxy poly(ethylene glycol) (PEG-MW 5.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 5000 DaFURTHER INFORMATION: -

References:

f W. Rapp, L. Zhang, A.G. Beck-Sickinger, K. Dares, K.-H. Wiesmüller,

G. Jung, E. Bayer; in Peptides 1990 Proceedings oft he 21st European

Peptide Symposium (E. Giralt and D. Andreu, Eds.); ESCOM, Leiden;

1991; 849.

f S. Butz, S. Rawer, W. Rapp, U. Birsner; Pept. Res. 1994; 7: 20.

f T.S. Burkoth, T.L.S. Benzinger, D.N.M. Jones, K. Hallenga, S.C.

Meredit, D.G. Lynn; J. Am. Chem. Soc. 1998; 120: 7655-7656.

f K.-H. Wiesmüller, G. Jung, G. Hess; Vaccine 1989; 7: 29.

f B. Kleine, W. Rapp, K.-H. Wiesmüller, M. Edinger, W. Beck, J.

Metzger, R. Ataullakhanov, G. Jung, W.G. Bessler; Immunology 1994;

110: 53.

f W. Rapp, L. Zhang, C. Müller, F. Zühl, K.-H. Woesmüller, G. Jung, E.

Bayer; in Innovations and Perspectives in Solid Phase Synthesis,

Peptides, Proteins and Nucleic Acids, Proceedings of the 3rd Interna-

tional Symposium 1993, (R. Epton, Ed.), Mayflower Worldwide Ltd.,

Birmingham, 1994; 197.





PEGylation modification with PEG carboxylic acids or PEG active esters is useful for improving water solubility, increasing chemical stability, decreasing aggregation and toxicity, and reduction of immunogenicity.

Amino protected amino-PEG-acids can be used for the PEGylation of solid particles, in order to create hydrophilic and reactive surfaces with no non-specific binding issues.

The amount of the PEG-NHS ester used in the modification reaction is potentially going to depend on several vari-ables, including:

a) the modification application, e.g., solution or surface, organic or aqueous, large biological or small organic,

b) the concentration of the specific reactive amines avail-able for reaction, as well as

c) the desired effect from the PEG which is incorporated.

In this latter case, choosing the proper length of the PEG will be important, and this may involve experimenting with different lengthes as well as a tribranched com-pounds. Therefore, these variables need to be taken into consideration before a basic optimization experiment is designed and run.

a) For aqueous based modifications the reaction can be run in an amine-free buffer at pH 7-8. The PEG NHS ester can be added as a stock solution in a dry organic solvent such as DMAC, DMSO or DMF. This stock solution can be stored for several months frozen at –20°C, if care is taken to exclude moisture in the preparation and handling of the NHS ester. The calculated amount of the stock is added to the aqueous reactant solution and the reaction will be complete in about 30 minutes to about 2 hours, depend-ing on the specific stoichiometry of the reaction and the desired extent of reaction. The half-life of the NHS ester depends on temperature, pH and structure, i.e. reactivity of the active ester (please see table). Use your established methods to monitor the reaction.

b) For organic based modifications standard organic procedures may be used, generally adding a solution of the PEG NHS ester to a solution of the reactant containing a tertiary amine, e.g., Hünig’s base, triethylamine or DBU. Homogeneous reactions are typically monitored by TLC or HPLC. Where possible methylene chloride as the reaction solvent is recommended, which also greatly facilitates the work-up. If the solubility of the compound to be modified will not allow this, other appropriate solvents like DMF or DMAC may be used. Optionally, the reaction can be run as slurry and the reaction will draw the reactants into solu-tion, as the incorporated PEG will significantly increase the solubility in many organic solvents, in particular in methylene chloride.

3.2 Amino-PeG-Acids and Active esters

Protocol for the Conjugation of Active Esters:

O

NH2 +PEG

O

N

O

O

NH

PEG

O




Protocol for in-situ Activation to the NhS ester:Add a methylene chloride solution of the acid to the dry reagents under dry conditions (10-20% molar excess of EDC and NHS in dry methylene chloride, dried over 3A molecular sieves). Stir for several hours or overnight, then evaporate the solvent and use. The reaction mixture can also be treated with a small amount of silica gel to adsorb the excess EDC and the urea by-product. Filter, then evaporate the solvent and use.

NHS should be added together with EDC to prevent for-mation of the anhydride. DCC and DIC can also be used. Typically use about 1 equivalent, and add a solution of the carbodiimide to the acid and NHS (1.1 to 1.2 eq.). PfOH (pentafluorophenol), MSNT (1-(Mesitylene-2-sulfonyl)-3-ni-

3.2.1 Aloc Protected Amino-PeG-Acids

AAA1905 Aloc-O2Oc-OH*DCHA AAA1905.0001 1 g € 90,00

AAA1905.0005 5 g € 350,00

AAA1905.0025 25 g € 1400,00NH O O OH

O

O

O

8-(Allyloxycarbonyl-amino)-3,6-dioxaoctanoic acid dicyclohexylamine, Aloc-Ado*DCHA, Aloc-AEEA*DCHA CAS-NO: 560088-74-6 FORMULA: C

10H

17NO

6*C

12H

23N

MOLECULAR WEIGHT: 247,11*181,32 g/moleFURTHER INFORMATION: -

tro-1,2,4-triazole), HOCt (Ethyl 1-hydroxy-1H-1,2,3-Triazole-4-carboxylate), HOPO (2-Hydroxypyridine-N-oxide) and a set of other coupling reagents/leaving groups can be used in place of NHS, if this is of any preference.

Reference:

f Greg T. Hermanson, Bioconjugate Techniques, 2nd Ed, Elsevier Inc.,

Burlington, MA 01803, April, 2008 (ISBN-13: 978-0-12-370501-3; ISBN-

10: 0-12-370501-0)., Ch. 18, pp. 711-742.


Structure of the Active Ester Corresponding Acidt1/2

[min]

pH 8 pH 7** pH 6**

PEG-O-CH2CH

2CH

2-CO

2-NHS Butyric acid 23.3 70 210

PEG-O-CO2-NHS Carbonate 20.4 61 183

PEG-O2C-CH

2-CH

2-CH

2-CO

2-NHS Glutaric acid 17.6 53 159

PEG-O-CH2CH

2-CO

2-NHS Propionic acid 16.5 49 147

PEG-S-CH2-CH

2-CO

2-NHS Mercaptopropionic acid 10.7 32 96

PEG-O2C-CH

2CH

2-CO

2-NHS Succinic acid 9.8 29 87

PEG-NH-CO-CH2CH

2-CO

2-NHS Succinamic acid 3.2 9 27

PEG-O-CH2-CO

2-NHS Acetic acid 0.75 2.25 6.75

Reactivity of PeG NhS Active esters towards Aminolysis* at 25°c:

* The relative reactivity of hydrolysis compared to aminolysis shows the same series, however, hydrolysis is much slower.

** calculated on basis of the data of pH8.

PEG acids can be activated in situ using standard activation methods, e.g., with EDC and NHS in methylene chloride:

HO

NH2 +PEG

O

NH

PEG

O+ NHS, EDC




3.2.2 Boc Protected Amino-PeG-AcidsBAA5240 Boc-O1Pen-OH*DCHA BAA5240.0005 5 g € 240,00

BAA5240.0025 25 g € 950,00

O NH

O

O

OH

O5-(t-Butyloxycarbonyl-amino)-3-oxapentanoic acid, [2-(Boc-amino)ethoxy]acetic acid, dicyclohexylamine CAS-NO: 142929-49-5 net FORMULA: C

9H

17NO

5*C

12H

23N


BAA6070 Boc,Pbf-amidino-O1Pen-OH BAA6070.0001 1 g € 100,00

BAA6070.0005 5 g € 400,00

BAA6070.0025 25 g € 1600,00N

OOH

NH

HN

OS

OO

O

O OBoc,Pbf-amidino-AEA, 5-[N-t-Butyloxycarbonyl-N‘-(2,2,4,6,7-pentame-thyldihydrobenzofuran-5-sulfonyl)]amidino-3-oxapentanoic acid, [2-(N-Boc-N‘-Pbf-amidino)ethoxy]acetic acid CAS-NO: 1263049-05-3 FORMULA: C

23H

35N

3O

8S


BAA1466 Boc-O2Oc-OH*DCHA BAA1466.0005 5 g € 200,00

BAA1466.0025 25 g € 800,00

NH O O OH

O

O

O

8-(t-Butyloxycarbonyl-amino)-3,6-dioxaoctanoic acid, 2,2-Dimethyl-4-oxo-3,8,11-trioxa-5-azatridecan-13-oic acid, {2-[2-(Boc-amino)ethoxy]ethoxy}acetic acid dicyclohexylamine, Boc-Ado, Boc-AEEA CAS-NO: 560088-79-1 FORMULA: C

11H

21NO

6*C

12H

23N


BAA6080 Boc,Pbf-amidino-O2Oc-OH BAA6080.0001 1 g € 100,00

BAA6080.0005 5 g € 400,00

BAA6080.0025 25 g € 1600,00

NO

O

NH

HN

S

OO

O

O O

OH

O

Boc,Pbf-amidino-Ado, Boc,Pbf-amidino-AEEA, 8-[N-t-Butyloxycarbonyl-N‘-(2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl)]amidino-3,6-dioxaoctanoic acid, {2-[2-(N-Boc-N‘-Pbf-amidino)ethoxy]ethoxy}acetic acid CAS-NO: 1263049-06-4 FORMULA: C

25H

39N

3O

9S


BAA1485 Boc-O2Oc-O2Oc-OH BAA1485.0001 1 g € 150,00

BAA1485.0005 5 g € 600,00

BAA1485.0025 25 g € 2400,00

O OHN

OO O OH

O

NH

O

O

17-(t-Butyloxycarbonyl-amino)-9-aza-3,6,12,15-tetraoxa-10-on-heptadecanoic acid CAS-NO: 1069067-08-8 FORMULA: C

17H

32N

2O

9


PEG1920 Boc-NH-dPEG™(4)-COOH PEG1920.0100 100 mg € 250,00

PEG1920.0001 1 g € 400,00

PEG1920.0005 5 g € 1000,00

OO

OO

HN

O

OH

O

O

15-t-Butyloxycarbonylamino-4,7,10,13-tetraoxa-pentadecanoic acid CAS-NO: FORMULA: C

16H

31NO

8

MOLECULAR WEIGHT: 365,42 g/moleFURTHER INFORMATION: Spacer is 17 atoms and 19.2 A

The general application of this heterobifunctional cross-linkers (NHS-dPEG™(4)-NHNH-Boc) is to react in a first step with its NHS function with an amine-containing target, followed by conjugating with a carbonyl containing complementary target molecule after the Boc hydrazide has been deprotected with either TFA or HCl.

Many biological molecules contain the amine function - or can have it incorporated - and the same can be said for the carbonyl moiety, in small molecule drugs, as well

as peptides, oligonucleotides or other complementary biologicals.

The main advantage of PEG containing heterobifunctional crosslinkers over conventional hydrophobic methylene spacers is that PEG spacers are very hydrophilic/water soluble and non-immunogenic spacers. These properties also can work to eliminate aggregation issues often encountered.





PEG1855 NHS-dPEG™(4)-NHNH-Boc PEG1855.0100 100 mg € 325,00

PEG1855.0001 1 g € 1000,00

NH

OO

OO

O

NH

HN O

O

O

O

O

N

O

O

1-(N‘-t-Butyloxycarbonyl)hydrazido-1,17-dioxo-4,7,10,13-tetraoxa-16-azahe-nicosan-21-oic acid succinimidyl ester CAS-NO: FORMULA: C

25H

42N

4O

12


PEG2410 Boc-NH-PEG(8)-COOH PEG2410.0100 100 mg € 275,00

PEG2410.0001 1 g € 700,00

OO OHN

HO

O

7

O

alpha-t-Butyloxycarbonylamino-omega-carboxy octa(ethylene glycol) CAS-NO: FORMULA: C

24H

47NO

12


PEG1071 Boc-NH-PEG(8)-COOH PEG1071.0001 1 g € 575,00

PEG1071.0005 5 g € 1975,00

O NH

OO

HN

O

O

OOH

O6

alpha-t-Butyloxycarbonylamino-omega-diglycolic acid octa(ethylene glycol) CAS-NO: FORMULA: C

25H

48N

2O

13


PEG2415 Boc-NH-PEG(12)-COOH PEG2415.0100 100 mg € 300,00

PEG2415.0001 1 g € 800,00

OO OHN

HO

O

11

O

alpha-t-Butyloxycarbonylamino-omega-carboxy dodeca(ethylene glycol) CAS-NO: FORMULA: C

32H

63NO

16


PEG1070 Boc-NH-PEG(12)-COOH PEG1070.0001 1 g € 575,00

PEG1070.0005 5 g € 1975,00

O NH

OO

HN

O

O

OOH

O10

alpha-t-Butyloxycarbonylamino-omega-[(aminocarboxymethoxy)acetic acid] dodecae(ethylene glycol) CAS-NO: FORMULA: C

33H

64N

2O

17



PEG4460.1000 1 g € 900,00

OO OHN

HO

O

15

O

alpha-t-Butyloxycarbonylamino-omega-carboxy hexadeca(ethylene glycol) CAS-NO: FORMULA: C

40H

79NO

20



PEG4470.1000 1 g € 1000,00

OO OHN

HO

O

19

O

alpha-t-Butyloxycarbonylamino-omega-carboxy 20(ethylene glycol) CAS-NO: FORMULA: C

48H

95NO

24

MOLECULAR WEIGHT: 1070,26 g/moleFURTHER INFORMATION: Spacer length 75.2 atoms or 64 A


PEG4480.1000 1 g € 1300,00

OO OHN

HO

O

23

O

alpha-t-Butyloxycarbonylamino-omega-carboxy 24(ethylene glycol) CAS-NO: FORMULA: C

56H

111NO

28







PEG4490.1000 1 g € 1450,00O

O OHNH

O

O

35

Oalpha-t-Butyloxycarbonylamino-omega-carboxy 36(ethylene glycol) CAS-NO: FORMULA: C

80H

159NO

40


PEG1073 Boc-NH-PEG-COOH PEG1073.0500 500 mg € 180,00

PEG1073.0001 1 g € 280,00

O NH

OO

O

n

OH

O

alpha-t-Butyloxycarbonylamino-omega-carboxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1074.0001 1 g € 280,00

O NH

OO

O

n

OH

O



PEG1072.0001 1 g € 350,00

O NH

OO

O

n

OH

O


PEG1111 Boc-NH-PEG-NHS PEG1111.0500 500 mg € 225,00

PEG1111.0001 1 g € 375,00O N

H

OO

O

n

O

O

N

O

O

alpha-t-Butyloxycarbonylamino-omega-carboxy succinimidyl ester poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1112.0001 1 g € 375,00O N

H

OO

O

n

O

O

N

O

O



PEG1110.0001 1 g € 450,00O N

H

OO

O

n

O

O

N

O

O



Need GMP production of PEGs? Please inquire!

O NH

OO

O

n

O

O

N

O

O

O NH

OO

O

n

OH

O




Dde Amino protected Compounds in Organic Synthesis

1. The Dde-protecting group is stable to Boc- and Trt-cleavage reagents (TFA), to Fmoc deprotecting reagents (Piperidine or DBU) and also Pd(0) for Aloc/All removal.

2. Dde can be removed with 2% hydrazine in DMF. However, in the presence of Aloc groups a partial reduction can occur (Rohwedder, B.; Mutti, Y.; Dumy, P.; Mutter. M.; Tetrahedron Lett. 1998; 39: 1175). In the presence of Fmoc groups these are readily deprot-ected! To selectively deprotect Dde in the presence of other protecting groups a mixture of NH

2OH*HCl/

Imidazole in NMP/DCM can be used (Díaz-Mochón, J.J.; Bialy, L.; Mark Bradley; Organic Letters 2004; 6(7): 1127-1129).

3. Dde-protected compounds are applied in solid-phase synthesis of peptides, polyamines and other com-pounds.

4. Side reactions with the Dde-group and its suppression are published in [3].

5. Suppressing side reactions with Aloc-group in the Dde-deprotection step can be found in [7]

Selective Deprotection Mixture according to Mark Bradley et al.:

1.25g (1.80 mmol) of NH2OH*HCl and 0.92g (1.35 mmol) of

imidazole were suspended in 5 mL NMP, and the mixture sonicated until complete dissolution. This solution can be stored for at least 2 weeks at -20°C. Just before reaction 5 volumes of this solution were diluted with 1 volume of alternatively DCM or DMF.

Published Applications:

f Mitsunobu alkylation with Dde-aminoalcohols; Dde-Tyr(ol) was noted as best protected derivative for the synthesis of chiral building blocks, [1].

f Dde-Phe(ol) [5] and Dde-NH-(CH2)3-OH, Dde-NH-(CH

2)4-

OH [20] were also used in solid-phase N-alkylation under Mitsunobu condition.

f Solid Phase syntheses of Lys derivatives [9], peptides and mimetics [4,10,12,14,15,16,17,18,19, 23, 26].

f Oligonucleotide-peptide hybrid [13].

f Glycopeptidolipids with Dde-protection [24].

f Dde-protected cysteine derivatives are used for the synthesis of asymmetric cystines [21].

DAA1016 Dde-O2Oc-OH DAA1016.0001 1 g € 125,00

DAA1016.0005 5 g € 450,00

DAA1016.0025 25 g € 1800,00NH

OO

OH

O

O

O

8-[(4,4-Dimethyl-2,6-dioxocyclohex-1-ylidene)ethyl-amino]-3,6-dioxaoc-tanoic acid, {2-[2-(Dde-amino)ethoxy]ethoxy}acetic acid CAS-NO: FORMULA: C

16H

25NO

6


Article No. Quantity Price3.2.3 Dde Protected Amino-PeG-Acids

1. P. Page, et al., JOC 1999; 64: 794.

2. Nash,et al., Tetr.Lett. 1996; 37(15): 2625.

3. K. Augustyns, et al., J.Peptide Res. 1998; 51: 127.

4. S.K. Sharma, et al., J.Peptide Res. 1999; 53: 501.

5. Fr. Berst, et al., Tetr.Lett. 2000; 41: 6649.

6. Cr.J. Leitheiser, et al., Org.Lett. 2000; 2(21): 3397.

7. B. Rohwedder, et al., Tetr.Lett. 1998; 39: 1175.

8. Fr. Berst, et al., Tetr.Lett. 2000; 41: 6649.

9. P.J. Connolly, et al., Tetr.Lett. 2000; 41: 5187.

10. St. Peluso, et al., JOC 1999; 64: 7114.

11. B. Kellam, et al., Tetr.Lett. 1997; 38: 4849.

12. D. Lelievre, et al., Tetr.Lett. 1995; 36: 9317.

13. J.-Chr. Truffert, et al., Tetr.Lett. 1994; 35: 2353.

14. G.B. Bloomberg, et al., Tetr.Lett. 1993; 34: 4709.

15. B.W. Bycroft, et al., J.Chem.Soc., Chem.Comm. 1993; 778.

16. N. Ahlborg, J.Immun.Meth. 1995; 179: 269.

17. J. Eichler, et al., Pept.Res. 1994; 7: 300.

18. C.G. Fields, et al., Biopolymers. 1993; 33: 1695.

19. P. Hoogerhout, et al., J.Pept.Res. 1999; 54: 436.

20. N.D. Hone, et al., Tetr.Lett., 2000; 41: 6149.

21. S. Zuberi, et al., Tetr.Lett. 1998; 39; 7567.

22. S.L. Mellor, et al., Tetr.Lett. 1997; 38: 3311.

23. S.S. Rahman, et al., JOC. 1998; 63: 6196.

24. F.Reichel, et al., JOC. 2000; 65: 3357.

25. N. Willand et al., Tetr. 2002; 58: 5741.

26. Gopalsamy, et al., Bioorg.med.chem.Lett. 2000; 10: 1715.

References:




PEG2145 Dnp-NH-PEG(4)-COOH PEG2145.0100 100 mg € 300,00

PEG2145.0001 1 g € 950,00

OO

OO

NH

O

OH

NO2

O2N

1-(2,4-Dinitrophenylamino)-3,6,9,12-tetraoxapentadecanoic acid CAS-NO: FORMULA: C

17H

25N

3O

10


PEG2285 Dnp-NH-PEG(12)-COOH PEG2285.0100 100 mg € 350,00

PEG2285.0001 1 g € 1200,00

OO OHN

H 11

O

NO2

O2Nalpha-(2,4-Dinitrophenyl)amino-omega-carboxy dodeca(ethylene glycol) CAS-NO: FORMULA: C

33H

57N

3O

18

MOLECULAR WEIGHT: 783,81 g/moleFURTHER INFORMATION: Spacer is 45 atoms and 50 A

PEG2150 Dnp-NH-PEG(4)-NHS PEG2150.0100 100 mg € 350,00

PEG2150.0001 1 g € 925,00

OO

OO

NH

O

O

NO2

O2N

N

O

O

1-(2,4-Dinitrophenylamino)-3,6,9,12-tetraoxapentadecanoic acid succi-nimidyl ester CAS-NO: FORMULA: C

21H

28N

4O

12


PEG2290 Dnp-NH-PEG(12)-NHS PEG2290.0100 100 mg € 375,00

PEG2290.0001 1 g € 1150,00

OO ON

H 11

O

NO2

O2N

N

O

O

alpha-(2,4-Dinitrophenyl)amino-omega-succinimidyl ester dodeca(ethylene glycol) CAS-NO: FORMULA: C

34H

60N

4O

20


⇒

see also our section about new PEG-based Dendrimers and Dendrons

regarding Hapten Carrier Molecules


Hapten-carrier for anti-DNP antibodies:

The DNP-PEGs can be used to label a carrier such as KLH for generating anti-DNP antibodies.

Find protocols for different conjugation agents at:



10: 0-12-370501-0). Chapter 19.

3.2.4 Dnp Protected Amino-PeG-Acids




3.2.5 Fmoc Protected Amino-PeG-Acids FAA1565 Fmoc-O1Pen-OH FAA1565.0001 1 g € 50,00

FAA1565.0005 5 g € 200,00

FAA1565.0025 25 g € 800,00O NH

OO

OH

O5-(9-Fluorenylmethyloxycarbonyl-amino)-3-oxapentanoic acid, [2-(Fmoc-amino)ethoxy]acetic acid CAS-NO: 260367-12-2 FORMULA: C

19H

19NO

5


FAA1435 Fmoc-O2Oc-OH FAA1435.0001 1 g € 85,00

FAA1435.0005 5 g € 200,00

FAA1435.0025 25 g € 800,00NHO

OOH

O

O

O

8-(9-Fluorenylmethyloxycarbonyl-amino)-3,6-dioxaoctanoic acid, {2-[2-(Fmoc-amino)ethoxy]ethoxy}acetic acid, 1-(9H-Fuoren-9-yl)-3-oxo-2,7,10-trioxa-4-azadodecan-12-oic acid, Fmoc-Ado, Fmoc-AEEA CAS-NO: 166108-71-0 FORMULA: C

21H

23NO

6


FAA6020 Fmoc-O2Oc-OPfp FAA6020.0001 1 g € 150,00

FAA6020.0005 5 g € 500,00

FAA6020.0025 25 g € 2000,00NHO

OO

O

O

O

FF

FF

F

8-(9-Fluorenylmethyloxycarbonyl-amino)-3,6-dioxaoctanoic acid pentafluorophenyl ester, {2-[2-(Fmoc-amino)ethoxy]ethoxy}acetic acid pentafluorophenyl ester, 1-(9H-Fuoren-9-yl)-3-oxo-2,7,10-trioxa-4-azado-decan-12-oic acid pentafluorophenyl ester, Fmoc-Ado- CAS-NO: 1263044-39-8 FORMULA: C

27H

22F

5NO

6


PEG1810 Fmoc-AEEP PEG1810.0001 1 g € 150,00

PEG1810.0005 5 g € 550,00

PEG1810.0025 25 g € 1750,00

HN

OOO

O

OH

O

3-(2-(2-(9-Fluorenylmethyloxycarbonyl)aminoethoxy)ethoxy)propanoic acid CAS-NO: 872679-70-4 FORMULA: C

22H

25NO

6


FAA1787 Fmoc-O2Oc-O2Oc-OH FAA1787.0001 1 g € 150,00

FAA1787.0005 5 g € 600,00

FAA1787.0025 25 g € 2400,00

OO

HN

OO

OOH

O

NH

O

O

17-(9-Fluorenylmethyloxycarbonyl-amino)-9-aza-3,6,12,15-tetraoxa-10-on-heptadecanoic acid, Fmoc-Ado-Ado-OH, Fmoc-AEEA-AEEA-OH CAS-NO: 560088-89-3 FORMULA: C

27H

34N

2O

9


FAA6790 Fmoc-O2Oc-O2Oc-OPfp FAA6790.0001 1 g € 300,00

FAA6790.0005 5 g € 1200,00

O OHN

OO O O

O

NH

O

O FF

F

FF

Fmoc-Ado-Ado-OPfp, Fmoc-AEEA-AEEA-OPfp, 17-(9-Fluorenylmethylo-xycarbonyl-amino)-9-aza-3,6,12,15-tetraoxa-10-on-heptadecanoic acid pentafluorophenyl ester CAS-NO: FORMULA: C

33H

33F

5N

2O

9


FAA1568 Fmoc-TTDS-OH FAA1568.0001 1 g € 100,00

FAA1568.0005 5 g € 400,00

OO

OHN

OH

O

O

HNO

O

[N1-(9-Fluorenylmethoxycarbonyl)-1,13-diamino-4,7,10-trioxatridecan-suc-

cinamic acid CAS-NO: FORMULA: C

29H

38N

2O

8


PEG4370 Fmoc-NH-dPEG™(3)-COOH PEG4370.1000 1 g € 400,00

PEG4370.5000 5 g € 1150,00

O NH

O OO

OOH

O

12-(9-Fluorenyloxycarbonylamino)-4,7,10-trioxa-dodecanoic acid CAS-NO: FORMULA: C

24H

29NO

7






PEG1820 Fmoc-NH-dPEG™(4)-COOH PEG1820.0100 100 mg € 250,00

PEG1820.0001 1 g € 400,00

PEG1820.0005 5 g € 1150,00

OO

OO

HN

O

OH

O

O

15-(9-Fluorenyloxycarbonyl)amino-4,7,10,13-tetraoxa-pentadecanoic acid CAS-NO: 557756-85-1 FORMULA: C

26H

33NO

8


PEG4410 Fmoc-NH-dPEG™(4)-NHS PEG4410.0100 100 mg € 275,00

PEG4410.1000 1 g € 425,00

3

O NH

OO O

OON

O

O

15-(9-Fluorenyloxycarbonyl)amino-4,7,10,13-tetraoxa-pentadecanoic acid succinimidyl ester CAS-NO: FORMULA: C

30H

36N

2O

10


PEG4380 Fmoc-NH-dPEG™(5)-COOH PEG4380.1000 1 g € 550,00

PEG4380.5000 5 g € 2100,00

4O N

HO O OH

OO18-(9-Fluorenyloxycarbonylamino)-4,7,10, 13-tetraoxa-octadecanoic acid CAS-NO: FORMULA: C

28H

37NO

9



PEG1825.0001 1 g € 525,00

PEG1825.0005 5 g € 1600,00NH

OO OH

O

O5

O1-(9-Fluorenylmethyloxycarbonyl)amino-3,6,9,12,15,18-hexaoxahenico-san-21-oic acid CAS-NO: FORMULA: C

30H

41NO

10



PEG1830.0001 1 g € 650,00

NH

OO OH

O

O7

O1-(9-Fluorenylmethyloxycarbonyl)amino-3,6,9,12,15,18,21,24-octaoxahep-tacosan-27-oic acid CAS-NO: FORMULA: C

34H

49NO

12



PEG4420.1000 1 g € 725,00

7

O NH

OO O

OON

O

O

alpha-(Fmoc-amino)-omega-(succinimidyl propionate) octa(ethylene glycol) CAS-NO: FORMULA: C

38H

52N

2O

14


PEG1080 Fmoc-NH-PEG(12)-COOH PEG1080.0100 100 mg € 400,00

PEG1080.0001 1 g € 750,00

PEG1080.0005 5 g € 2400,00NH

OO OH

O

O11

O1-(9-Fluorenylmethyloxycarbonyl)amino-3,6,9,12,15,18,21,24,27,30,33,36-dodecaoxanonatriacontan-39-oic acid CAS-NO: 867062-95-1 FORMULA: C

42H

65NO

16



PEG4430.1000 1 g € 800,00

11

O NH

OO O

OON

O

O

alpha-(Fmoc-amino)-omega-(succinimidyl propionate) dodeca(ethylene glycol) CAS-NO: FORMULA: C

46H

68N

2O

18






PEG4670 Fmoc-NH-O-dPEG™(12)-COOH PEG4670.0100 100 mg € 450,00

PEG4670.1000 1 g € 1275,00

12O

O OH

O

HNO

O

alpha-(9-Fluorenylmethyloxycarbonyl-aminoxy)-omega-(propionic acid)-dodeca(ethylene glycol) CAS-NO: FORMULA: C

42H

65NO

17

MOLECULAR WEIGHT: 39072091 g/moleFURTHER INFORMATION: -

PEG4630 Phth-NO-dPEG™(12)-NHS PEG4630.0100 100 mg € 475,00

PEG4630.1000 1 g € 1350,00

12

NO

O ON

O

O

O

OO

alpha-Pthaloylaminoxy-omega-(succinimidyl propionate)-dodeca(ethylene glycol) CAS-NO: FORMULA: C

39H

60N

2O

19


PEG3180 Fmoc-NH-PEG(16)-COOH PEG3180.0100 100 mg € 350,00

PEG3180.1000 1 g € 750,00

NH

OO OH

O

O15

Oalpha-(9-Fluorenylmethyloxycarbonyl)amino-omega-carboxy hexadeca(ethylene glycol) CAS-NO: FORMULA: C

50H

81NO

20



PEG4390.1000 1 g € 1000,00

19O N

HO O OH

OOalpha-Fmoc-amino-20(ethylene glycol)-omega-carboxylic acid CAS-NO: FORMULA: C

58H

97NO

24



PEG1815.0001 1 g € 1300,00NH

OO OH

O

O23

Oalpha-Fmoc-amino-24(ethylene glycol)-omega-carboxylic acid CAS-NO: FORMULA: C

66H

113NO

28


PEG1210 Fmoc-NH-PEG(27)-COOH PEG1210.0001 1 g € 900,00

PEG1210.0005 5 g € 3250,00

NH

OO OH

O

O27

Oalpha-(9-Fluorenylmethyloxycarbonyl)amino-27(ethylene glycol)-omega-propionic acid CAS-NO: FORMULA: C

74H

129NO

32



PEG4400.1000 1 g € 1450,00

35O N

HO O OH

OOalpha-Fmoc-amino-36(ethylene glycol)-omega-carboxylic acid CAS-NO: FORMULA: C

90H

161NO

40






PEG1108 Fmoc-NH-PEG-COOH PEG1108.0500 500 mg € 200,00

PEG1108.0001 1 g € 350,00

PEG1108.0005 5 g € 1500,00O NH

OO

O

n

OH

O

alpha-(9-Fluorenylmethyloxycarbonyl)amino-omega-carboxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1109.0001 1 g € 350,00

PEG1109.0005 5 g € 1500,00O NH

OO

O

n

OH

O



PEG1107.0001 1 g € 400,00

O NH

OO

O

n

OH

O


PEG1117 Fmoc-NH-PEG-NHS PEG1117.0500 500 mg € 220,00

PEG1117.0001 1 g € 375,00

O NH

OO

O

n

O

O

N

O

O

alpha-(9-Fluorenylmethyloxycarbonyl)amino-omega-carboxy succinimi-dyl ester poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1118.0001 1 g € 375,00

O NH

OO

O

n

O

O

N

O

O



PEG1116.0001 1 g € 440,00

O NH

OO

O

n

O

O

N

O

O



O NH

OO

O

n

OH

O

O NH

OO

O

n

O

O

N

O

O





Useful for incorporating a protected amine, whose protect-ing group is orthogonal to Fmoc strategy. The PEGylation spacer increases water solubility, provides non-immuno-genicity, and non-aggregating properties.

Mmt can be removed under mild conditions, for example using very low concentrations of TFA (trifluoroacetic acid), hexafluoroisopropanol or 20% TFE (trifluoroethanol) in methylene choride. Acids need to be activated to the ac-tive ester with e.g. EDC or DCC, NHS, or PfOH.

References:

f G.M. Dubowchik and S. Rakia, Tetrahedron Letters 1997; 38(30): 5257-5260.

f S. Matysiak, et al., Tetrahedron Letters 1998, 39: 1733-1734.

f D. W. Will, et al., Tetrahedron 1995; 51(44): 12069-12082.

f A. Aletras, et al., Int. J. Peptide Protein Res. 1995; 45: 488-496.

PEG4650 Mtt-O2Oc-OH*DEA PEG4650.0001 1 g € 200,00

PEG4650.0005 5 g € 800,00

PEG4650.0025 25 g € 3200,00NH

OO

OH

O

Me

N-(4-Methyltrity)-8-amino-3,6-dioxaoctanoic acid diethylamine CAS-NO: FORMULA: C

26H

29NO

4*C

4H

11N


PEG2160 Mmt-NH-PEG(4)-COOH PEG2160.0100 100 mg € 275,00

PEG2160.0001 1 g € 425,00

OO

OO

NH

O

OHMeO

1-(p-Methoxytritylamino)-3,6,9,12-tetraoxapentadecanoic acid CAS-NO: FORMULA: C

31H

39NO

7

MOLECULAR WEIGHT: 537,64 g/moleFURTHER INFORMATION: Space is 28 atoms and 32.2

PEG2385 Mmt-NH-PEG(4)-CO-OPfp PEG2385.0100 100 mg € 275,00

PEG2385.0001 1 g € 450,00O

O ONH 3

O

MeO

F

F

F

F

F

15-(p-Methoxytritylamino)-4,7,10,13-tetraoxa-pentadecanoic acid penta-fluorphenyl ester CAS-NO: FORMULA: C

37H

38F

5NO

7


PEG4500 Mmt-NH-dPEG™(4)-TFP PEG4500.0100 100 mg € 250,00

PEG4500.1000 1 g € 450,00O

O ONH 3

O

MeO

F

F

F

F

15-(p-Methoxytritylamino)-4,7,10,13-tetraoxa-pentadecanoic acid 2,3,5,6-tetrafluorphenyl ester CAS-NO: FORMULA: C

37H

39F

4NO

7


MAA1010 Mmt-TTDS-OH MAA1010.0001 1 g € 100,00

MAA1010.0005 5 g € 400,00

OO

OHN

OH

O

O

HN

OMe

[N1-(4-Methoxytrityl)-1,13-diamino-4,7,10-trioxatridecan-succinamic acid

CAS-NO: FORMULA: C34

H44

N2O

7



PEG2265.0001 1 g € 700,00O

O OHNH 7

O

MeOalpha-p-Methoxytritylamino-omega-carboxy octa(ethylene glycol) CAS-NO: FORMULA: C

38H

55NO

11



3.2.6 Mtt and Mmt Protected Amino-PeG-Acids






PEG2390.0001 1 g € 870,00O

O ONH 7

O

MeO

F

F

F

F

F

alpha-p-Methoxytritylamino-omega-carboxy pentafluorphenyl ester octa(ethylene glycol) CAS-NO: FORMULA: C

45H

54F

5NO

11



PEG4510.1000 1 g € 750,00O

O ONH 7

O

MeO

F

F

F

F

alpha-p-Methoxytritylamino-omega-(2,3,5,6-tetrafluorphenyl propiona-te) octa(ethylene glycol) CAS-NO: FORMULA: C

45H

55F

4NO

11



PEG2270.0001 1 g € 800,00OO OHN

H 11

O

MeO

alpha-p-Methoxytritylamino-omega-carboxy dodeca(ethylene glycol) CAS-NO: FORMULA: C

47H

71NO

15



PEG2395.0001 1 g € 1050,00O

O ONH 11

O

MeO

F

F

F

F

F

alpha-p-Methoxytritylamino-omega-carboxy pentafluorphenyl ester dodeca(ethylene glycol) CAS-NO: FORMULA: C

53H

70F

5NO

15



PEG4520.1000 1 g € 900,00O

O ONH 11

O

MeO

F

F

F

F

alpha-p-Methoxytritylamino-omega-(2,3,5,6-tetrafluorphenyl propiona-te) dodeca(ethylene glycol) CAS-NO: FORMULA: C

53H

71F

4NO

15



PEG2275.0001 1 g € 950,00O

O OHNH 15

O

MeO

alpha-p-Methoxytritylamino-omega-carboxy hexadeca(ethylene glycol) CAS-NO: FORMULA: C

55H

87NO

19

MOLECULAR WEIGHT: 1066,27 g/moleFURTHER INFORMATION: Space is 52 atoms and 60.4 A


PEG2400.0001 1 g € 1230,00O

O ONH 15

O

MeO

F

F

F

F

F

alpha-p-Methoxytritylamino-omega-carboxy pentafluorphenyl ester hexadeca(ethylene glycol) CAS-NO: FORMULA: C

61H

86F

5NO

19



PEG4530.1000 1 g € 1000,00O

O ONH 15

O

MeO

F

F

F

F

alpha-p-Methoxytritylamino-omega-(2,3,5,6-tetrafluorphenyl propiona-te) hexadeca(ethylene glycol) CAS-NO: FORMULA: C

61H

87F

4NO

19







PEG4540.1000 1 g € 1200,00O

O ONH 19

O

MeO

F

F

F

F

alpha-p-Methoxytritylamino-omega-(2,3,5,6-tetrafluorphenyl propiona-te) 20(ethylene glycol) CAS-NO: FORMULA: C

69H

103F

4NO

23



PEG2280.0001 1 g € 1300,00O

O OHNH 23

O

MeO

alpha-p-Methoxytritylamino-omega-carboxy 24(ethylene glycol) CAS-NO: FORMULA: C

71H

119NO

27



PEG2405.0001 1 g € 1650,00O

O ONH 23

O

MeO

F

F

F

F

F

alpha-p-Methoxytritylamino-omega-carboxy pentafluorphenyl ester 24(ethylene glycol) CAS-NO: FORMULA: C

77H

118F

5NO

27



PEG4550.1000 1 g € 1400,00O

O ONH 23

O

MeO

F

F

F

F


77H

119F

4NO

27



PEG4560.1000 1 g € 1450,00O

O ONH 35

O

MeO

F

F

F

F


101H

167F

4NO

39


Spacer will enhance the water solubility, minimize or eliminate aggregation problems with its incorporation into peptides and related compounds. The spacer is also non-immunogenic.

Used for coating of beads or nanoparticles in order to reduce nonspecific binding problems. Can be activated via standard coupling chemistries, as the amine reacts unspecifically with NHS and other active esters in the presence of a tertiary amine, e.g., TEA.

Acids are zwitterionic, extremely water soluble, soluble in methylene chloride, soluble in other organic solvents of moderate polarity.

t-Butyl esters easily can be saponified with TFA (25% TFA in DCM, 0°C, 5 h).

t-Butyl group provides a potentially powerful purifica-tion handle due to its hydrophobicity. After normal phase chromatographic purification (e.g., silica gel) it can be removed to perform additional chemistry.

t-Butyl group neutralizes the zwitterion of the amino acid for better reactivity at the amine.

3.2.7 N-Unprotected Amino-PeG-Acids and esters





Amino-PEG-acids can be applied to surfaces as well as particles. The carboxylic acid density on the surface can be reduced by co-coating with mPEG-amines, which are generally equal or shorter than the amino-PEG-acids.

General protocols for reactions with active esters:Dissolve the active ester in an appropriate dry solvent (methylene chloride is preferred), add triethylamine and then the PEG-amine, either neat or drop wise as a solution in the reaction solvent. Use at least a 10% excess of all reagents rela-tive to the active ester. This can be carried out at ambient temperatures.

General protocols for reactions with free acids:1. Generate the active ester in situ with EDC and NHS, then add the TEA, followed by the amino-PEG-t-butyl ester; or

2. Combine acid, NHS, TEA, and the amino-PEG-t-butyl ester, and add a solution of EDC. Use at least 10% excess of reagents relative to the acid. Other Carbodiimides than EDC can be used, but the high water solubility and polar nature of the urea end product makes work-up very efficient with EDC compared to DIC or DCC. Normal reaction temperatures are -10°C to 0°C. Monitoring by chromatography (TLC or HPLC) is essential.

HN

O

O

O

O

O

HOO

HN

O

O

O

O

O

HN

O

O

O

O

O

HOO

HN

O

O

O

O

O

HN

O

O

O

O

O

HO

O

HN

O

O

O

O

O

HN

O

O

O

O

O

HN

O

O

O

O

O

HO

O

HN

O

O

O

O

O

HN

O

O

O

O

O

HO

O

HN

O

O

O

O

O

HN

O

O

O

O

O

OH

O

HN

O

O

O

O

O

HO O

+ PEGO

O

N

O

O

O

OtBu

H2NPEGN

H

OO

OtBu

+ PEGOH

OO

OtBu

H2NPEGN

H

OO

OtBu

EDC, NHS

References:

f Greg T. Hermanson, Bioconjugate Techniques, 2nd Ed, Elsevier Inc., Burlington, MA 01803, April, 2008 (ISBN-13: 978-0-12-370501-3; ISBN-10: 0-12-

370501-0). Chapter 14, pp. 582-626.




PEG1365 H2N-EG2-CO-OtBu PEG1365.0100 100 mg € 250,00

PEG1365.0001 1 g € 475,00

OOO

H2N

O3-(2-(2-Aminoethoxy)ethoxy)propanoic acid t-butyl ester CAS-NO: FORMULA: C

11H

23NO

4


PEG2420 H-O2Oc-OH PEG2420.0001 1 g € 90,00

PEG2420.0005 5 g € 350,00

PEG2420.0025 25 g € 1400,00NH2

OO

OH

O

AEEA, H-Ado-OH, 8-amino-3,6-dioxaoctanoic acid CAS-NO: 134978-97-5 FORMULA: C

6H

13NO

4


PEG2430 H-O2Oc-OtBu*HCI PEG2430.0001 1 g € 300,00

PEG2430.0005 5 g € 1200,00NH2

OO

O

O

AEEA-OtBu*HCI, H-Ado-OtBu*HCI, 8-amino-3,6-dioxaoctanoic acid t-butyl ester hydrochloride CAS-NO: 251564-45-1 net FORMULA: C

10H

21NO

4*HCI


PEG1221 H-O2Oc-O2Oc-OH PEG1221.0001 1 g € 400,00

PEG1221.0005 5 g € 1400,00

NHO

OOH

O

O

OO

H2N

H-AEEA-AEEA-OH, (AEEA)2, H-Ado-Ado-OH, 8-amino-3,6-dioxaoctanoic acid dimer, 17-Amino-10-oxo-3,6,12,15-tetraoxa-9-azaheptadecan-1-oic acid CAS-NO: 1143516-05-5 FORMULA: C

12H

24N

2O

7


PEG2770 H-O2Oc-O2Oc-O2Oc-OH PEG2770.0250 250 mg € 175,00

PEG2770.0001 1 g € 500,00

PEG2770.0005 5 g € 2000,00

NHO

O

HN

O

O

OO

H2NO

OOH

O

H-AEEA-AEEA-AEEA-OH, (AEEA)3, H-Ado-Ado-Ado-OH, 8-amino-3,6-dioxaoctanoic acid trimer, 26-amino-10,19-dioxo-3,6,12,15,21,24-hexao-xa-9,18-diazahexacosan-1-oic acid CAS-NO: FORMULA: C

18H

35N

3O

10


PEG1370 H2N-dPEG™(4)-COOH PEG1370.0100 100 mg € 250,00

PEG1370.0001 1 g € 600,00O

OO

OH2N

O

OH15-Amino-4,7,10,13-tetraoxa-pentadecanoic acid CAS-NO: FORMULA: C

11H

23NO

6


PEG1375 H2N-dPEG™(4)-CO-OtBu PEG1375.0100 100 mg € 275,00

PEG1375.0001 1 g € 750,00O

OO

OH2N

O

O15-Amino-4,7,10,13-tetraoxa-pentadecanoic acid t-butyl ester CAS-NO: FORMULA: C

15H

31NO

6



PEG1300.0001 1 g € 600,00

H2NO

OO

OO

O OH

O1-Amino-3,6,9,12,15,18-hexaoxahenicosan-21-oic acid CAS-NO: FORMULA: C

15H

31NO

8







PEG1305.0001 1 g € 750,00

H2NO

OO

OO

O O

O

1-Amino-3,6,9,12,15,18-hexaoxahenicosan-21-oic acid t-butyl ester CAS-NO: FORMULA: C

19H

39NO

8



PEG1380.0001 1 g € 850,00

OHOO

H2N7

O1-Amino-3,6,9,12,15,18,21,24-octaoxaheptaeicosane-27-oic acid CAS-NO: FORMULA: C

19H

39NO

10



PEG1385.0001 1 g € 800,00H2N

OO O

O7

1-Amino-3,6,9,12,15,18,21,24-octaoxaheptaeicosane-27-oic acid t-butyl ester CAS-NO: FORMULA: C

23H

47NO

10



PEG1345.0001 1 g € 1000,00H2N

OO OH

O11

1-Amino-3,6,9,12,15,18,21,24,27,30,33,36-dodecaoxanonatriacontan-39-oic acid CAS-NO: FORMULA: C

27H

55NO

14



PEG1350.0001 1 g € 850,00H2N

OO O

O11

1-Amino-3,6,9,12,15,18,21,24,27,30,33,36-dodecaoxanonatriacontan-39-oic acid t-butyl ester CAS-NO: FORMULA: C

31H

63NO

14



PEG3320.1000 1 g € 1100,00H2NO

O OH

O15

alpha-Amino-omega-propionic acid-16(ethylen glycol) CAS-NO: FORMULA: C

35H

71NO

18



PEG3690.1000 1 g € 1000,00H2NO

O O

O15

alpha-Amino-omega-(t-butyl propionate) hexadeca(ethylene glycol) CAS-NO: FORMULA: C

39H

79NO

18



PEG3330.1000 1 g € 1200,00H2NO

O OH

O19


43H

87NO

22







PEG3700.1000 1 g € 1150,00H2N

OO O

O19

alpha-Amino-omega-(t-butyl propionate) 20(ethylene glycol) CAS-NO: FORMULA: C

47H

95NO

22



PEG1355.0001 1 g € 1150,00H2N

OO OH

O

23

alpha-Amino-24(ethylene glycol)-omega-propionic acid CAS-NO: FORMULA: C

51H

103NO

26



PEG1360.0001 1 g € 1100,00H2N

OO O

O

23

alpha-Amino-24(ethylene glycol)-omega-propionic acid t-butyl ester CAS-NO: FORMULA: C

55H

111NO

26



PEG3340.1000 1 g € 1450,00H2NO

O OH

O35


75H

151NO

38



PEG3710.1000 1 g € 1450,00H2NO

O O

O35

alpha-Amino-omega-(t-butyl propionate) 36(ethylene glycol) CAS-NO: FORMULA: C

79H

159NO

38


PEG1096 H2N-PEG-COOH*HCl PEG1096.0500 500 mg € 180,00

PEG1096.0001 1 g € 325,00

H2NO

O

n

OH

O

alpha-Amino-omega-carboxy poly(ethylene glycol) hydrochloride (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1097.0001 1 g € 325,00

H2NO

O

n

OH

O



PEG1095.0001 1 g € 375,00

H2NO

O

n

OH

O



H2NO

O

n

OH

O





PEG4710 Z-O1Pen-OH PEG4710.0005 5 g € 300,00

PEG4710.0025 25 g € 1200,00

O NH

OOH

O O5-(Benzyloxycarbonyl-amino)-3-oxa-pentanoic acid CAS-NO: FORMULA: C

12H

5NO

5


ZAA1186 Z-O2Oc-OH*DCHA ZAA1186.0001 1 g € 85,00

ZAA1186.0005 5 g € 225,00

ZAA1186.0025 25 g € 900,00NHO

OOH

O

O

O

8-(Benzyloxycarbonyl-amino)-3,6-dioxaoctanoic acid dicyclohexylami-ne, Z-Ado*DCHA, Z-AEEA*DCHA CAS-NO: 560088-84-8 FORMULA: C

14H

19NO

6*C

12H

23N

MOLECULAR WEIGHT: 297,31*181,32 g/mole

PEG1495 Z-NH-dPEG™(4)-COOH PEG1495.0100 100 mg € 275,00

PEG1495.0001 1 g € 425,00

OO

OO

HN

O

OHO

O

15-Benzyloxycarbonylamino-4,7,10,13-tetraoxa-pentadecanoic acid CAS-NO: FORMULA: C

19H

29NO

8



PEG1795.0001 1 g € 650,00OHOO

HNO

O 5 O

1-Benzyloxycarbonylamino-3,6,9,12,15,18-hexaoxahenicosan-21-oic acid CAS-NO: FORMULA: C

23H

37NO

10



PEG1800.0001 1 g € 650,00OHO

O

HNO

O 7 O

1-Benzyloxycarbonylamino-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-oic acid CAS-NO: FORMULA: C

27H

45NO

12

MOLECULAR WEIGHT: 575,65 g/moleFURTHER INFORMATION: Spacer is 28 atoms and 32.2


PEG1785.0001 1 g € 750,00OHO

O

HNO

O 11 O

1-Benzyloxycarbonylamino-3,6,9,12,15,18,21,24,27,30,33,36-do-decaoxanonatriacontan-39-oic acid CAS-NO: FORMULA: C

35H

61NO

16



PEG4570.1000 1 g € 900,00OHO

O

HNO

O 15 O

alpha-Benzyloxycarbonylamino-hexadeca(ethylene glycol)-omega-carboxylic acid CAS-NO: FORMULA: C

43H

77NO

20



PEG4580.1000 1 g € 1100,00OHO

O

HNO

O 19 O

alpha-Benzyloxycarbonylamino-amino-20(ethylene glycol)-omega-carboxylic acid CAS-NO: FORMULA: C

51H

93NO

24


3.2.8 Z Protected Amino-PeG-AcidsFor incorporating a PEG unit using standard Cbz-chemistry either as a spacer or terminal group in peptide sequences, typically used in solution synthesis.

The Cbz or Z protecting group is being deprotected by

hydrogenolysis using catalytic Pd/C.

PEG spacer provides water solubility, reduces or elimi-nates aggregation, and is inherently non-immunogenic and non-toxic.






PEG1790.0001 1 g € 1300,00NH

OO OH

O

23

O

Oalpha-Benzyloxycarbonylamino-24(ethylene glycol)-omega-propionic acid CAS-NO: FORMULA: C

59H

109NO

28



PEG4590.1000 1 g € 1450,00OHO

O

HNO

O 35 O

alpha-Benzyloxycarbonylamino-amino-36(ethylene glycol)-omega-carboxylic acid CAS-NO: FORMULA: C

83H

157NO

40


3.3 PeG-Acids carrying various other terminal Groups3.3.1 Formyl-PeG-esters PEG4690 FB-dPEG™(12)-TFP PEG4690.0100 100 mg € 425,00

PEG4690.1000 1 g € 1325,0012

NH

O O

O

O

H

O

F

F

F

F

alpha-(p-Formylbenzoylamido)-omega-[(2,3,5,6-tetrafluorophenyl)propionate]-dodeca(ethylene glycol) CAS-NO: FORMULA: C

41H

59F

4NO

16


PEG4700 FB-dPEG™(24)-TFP PEG4700.0100 100 mg € 475,00

PEG4700.1000 1 g € 1600,0024

NH

O O

O

O

H

O

F

F

F

F

alpha-(p-Formylbenzoylamido)-omega-[(2,3,5,6-tetrafluorophenyl)propionate]-24(ethylene glycol) CAS-NO: FORMULA: C

65H

107F

4NO

28


3.3.2 Acryloyl-PeG-esters PEG1223 ACRL-PEG-NHS PEG1223.0500 500 mg € 1500,00

PEG1223.0001 1 g € 2500,00NH

OO

n

O

O

N

O O

O

alpha-Acryloyl-omega-carboxy succinimidyl ester poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da

PEG1224 ACRL-PEG-NHS PEG1224.0500 500 mg € 1500,00

PEG1224.0001 1 g € 2500,00NH

OO

n

O

O

N

O O

O


PEG1222 ACRL-PEG-NHS PEG1222.0500 500 mg € 1500,00

PEG1222.0001 1 g € 2500,00NH

OO

n

O

O

N

O O

O


α Other Acryloyl-PEG derivatives available on custom synthesis basis.


NH

OO

n

O

O

N

O O

O




3.3.3 epoxy-PeG-Acids PEG1208 Epoxy-PEG-COOH PEG1208.0500 500 mg € 1750,00

PEG1208.0001 1 g € 2500,00

OO

NH

n

OH

O

O

O

alpha-Epoxy-omega-carboxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -

3.3.4 hydroxy-PeG-Acids

Can be used as starting material to make a variety of other functional PEG based compounds.

Surface modification reagent with free alcohol, which can be reacted with activated surfaces or converted to other reactive functionality.

PEG spacers are hydrophilic, water soluble and non-immunogenic, and will incorporate these properties into any application.

PEG1535 HO-dPEG™(4)-CO-OtBu PEG1535.0100 100 mg € 300,00

PEG1535.0001 1 g € 475,00O

OO

OHO

O

O15-Hydroxy-4,7,10,13-tetraoxa-pentadecanoic acid t-butyl ester CAS-NO: FORMULA: C

15H

30O

7


PEG1925 Bzl-O-dPEG™(4)-COOH PEG1925.0100 100 mg € 325,00

PEG1925.0001 1 g € 850,00O

OO

OO

O

OH

17-Phenyl-4,7,10,13,16-pentaoxa-heptadecanoic acid CAS-NO: FORMULA: C

18H

28O

7


PEG2355 HO-PEG(6)-CO-OtBu PEG2355.0100 100 mg € 300,00

PEG2355.0001 1 g € 600,00O

OHO5

O

Oalpha-Hydroxy-omega-carboxy t-butyl ester hexa(ethylene glycol) CAS-NO: FORMULA: C

19H

38O

9


PEG1540 HO-dPEG™(8)-CO-OtBu PEG1540.0100 100 mg € 325,00

PEG1540.0001 1 g € 625,00

OO

OO

HOO

OO

O O

O

t-Butyl 1-hydroxy-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-oate CAS-NO: FORMULA: C

23H

46O

11


PEG1090 HO-PEG(12)-CO-OtBu PEG1090.0001 1 g € 300,00

PEG1090.0005 5 g € 975,00O

OHO11

O

Oalpha-Hydroxy-omega-t-butyl propionat dodecae(ethylene glycol) CAS-NO: FORMULA: C

31H

62O

15


α Other Epoxy-PEG derivatives available on custom synthesis basis.





PEG3720 HO-dPEG™(16)-COOH PEG3720.0100 100 mg € 350,00

PEG3720.1000 1 g € 800,00

HOO O

O16

alpha-Hydroxy-omega-(t-butyl propionate) hexadecae(ethylene glycol) CAS-NO: FORMULA: C

39H

78O

19


PEG3730 HO-dPEG™(20)-COOH PEG3730.0100 100 mg € 400,00

PEG3730.1000 1 g € 950,00

HOO O

O20

alpha-Hydroxy-omega-(t-butyl propionate) 20(ethylene glycol) CAS-NO: FORMULA: C

47H

94O

23


PEG2365 HO-PEG(24)-CO-tBu PEG2365.0100 100 mg € 400,00

PEG2365.0001 1 g € 1000,00O

OHO23

O

Oalpha-Hydroxy-omega-carboxy t-butyl ester 24(ethylene glycol) CAS-NO: FORMULA: C

55H

110O

27


PEG1093 HO-PEG-COOH PEG1093.0500 500 mg € 140,00

PEG1093.0001 1 g € 200,00

HOO

NH

n

OH

O

Oalpha-Hydroxy-omega-carboxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1094.0001 1 g € 200,00

HOO

NH

n

OH

O



PEG1092.0001 1 g € 250,00

HOO

NH

n

OH

O



HOO

NH

n

OH

O

O





PEG1990 DIG(NHS)2 PEG1990.0001 1 g € 95,00

PEG1990.0005 5 g € 300,00

PEG1990.0025 25 g € 1200,00N

OO

ON

OOO

O

O

O

Bis-N-succinimidyl diglycolic acid, 2,2‘-Oxydiacetic acid bis-N-succini-midyl ester CAS-NO: 373614-12-1 FORMULA: C

12H

12N

2O

9


PEG1985 DIG(Pfp)2 PEG1985.0001 1 g € 90,00

PEG1985.0005 5 g € 350,00

PEG1985.0025 25 g € 1400,00OO

O

OOF

F

F

F

F

F

F

F

F

F

Bis-pentafluorophenyl diglycolic acid, 2,2‘-Oxydiacetic acid bis-penta-fluorophenyl ester CAS-NO: 158573-58-1 FORMULA: C

16H

4F

10O

5


PEG2035 DOODA PEG2035.0005 5 g € 200,00

PEG2035.0025 25 g € 600,00O

OOH

O

HO

O

3,6-Dioxaoctandioic acid CAS-NO: 23243-68-7 FORMULA: C

6H

10O

6

MOLECULAR WEIGHT: 178,14 g/moleFURTHER INFORMATION: Spacer is 10s atoms and 11.0 A

PEG4120 NHS-DOODA-NHS PEG4120.0100 100 mg € 275,00

PEG4120.1000 1 g € 700,00O

O OO

N

O

O

NO

O

O

O

3,6-Dioxaoctandioic acid bissuccinimidyl ester CAS-NO: FORMULA: C

16H

20N

2O

10


PEG4020 Pfp-DOODA-Pfp PEG4020.0100 100 mg € 275,00

PEG4020.1000 1 g € 700,00O

O OO

O

O

F

F

F

F

F

F

F

F

F

F

3,6-Dioxaoctandioic acid bispentafluorphenyl ester CAS-NO: FORMULA: C

20H

12F

10O

6


PEG2030 TUDA PEG2030.0025 25 g € 90,00

PEG2030.0100 100 g € 290,00O

OOH

O

OHO

O3,6,9-Trioxaundecandioic acid CAS-NO: 13887-98-4 FORMULA: C

8H

14O

7


PEG4130 NHS-TUDA-NHS PEG4130.0100 100 mg € 275,00

PEG4130.1000 1 g € 700,00OO O

ON

2

O

O

NO

O

O

O

3,6,9-Trioxaundecandioic acid bissuccinimidyl ester CAS-NO: FORMULA: C

18H

24N

2O

11


PEG4030 Pfp-TUDA-Pfp PEG4030.0100 100 mg € 275,00

PEG4030.1000 1 g € 700,00O

O OO

2

O

O

F

F

F

F

F

F

F

F

F

F

3,6,9-Trioxaundecandioic acid bispentafluorphenyl ester CAS-NO: FORMULA: C

22H

16F

10O

7


3.3.5 PeG-Di-(carboxylic Acids)

Homobifunctional amine reactive PEG crosslinker.

Used as “heterobifunctional” label for amine functionalized surfaces, including nanoparticles and cells.

Extremely hydrophilic and non-immunogenic.

The Bis-PEG-acid can be coupled using standard in situ activation methods, e.g., EDC and NHS in methylene chloride.

The Pfp esters react with amines in the same way as do the NHS esters, yet are more stable in aqueous solution than the NHS esters.

Reference:



10: 0-12-501-0), 235-274 and 711-714.





PEG3170 HOOC-PEG(3)-COOH PEG3170.0250 250 mg € 200,00

PEG3170.0001 1 g € 600,00

PEG3170.0005 5 g € 2400,00HOO

OOH

O

O3

3,6,9,12-Tetraoxatetradecane-1,14-dioic acid CAS-NO: 32775-08-9 FORMULA: C

10H

18O

8


PEG3960 NHS-dPEG™(4)-NHS PEG3960.0100 100 mg € 275,00

PEG3960.1000 1 g € 700,00O

O OO

N3

O

O

NO

O

O

O

Bis-succinimidyl-4,7,10,13-tetraoxahexadecane-1,16-dioate CAS-NO: FORMULA: C

20H

28N

2O

12


PEG4040 Pfp-dPEG™(3)-Pfp PEG4040.0100 100 mg € 275,00

PEG4040.1000 1 g € 700,00O

O OO

3

O

O

F

F

F

F

F

F

F

F

F

F

alpha,omega-Bis(pentafluorphenyl propionate) tri(ethylene glycol) CAS-NO: FORMULA: C

24H

20F

10O

8


PEG1430 HOOC-PEG(4)-COOH PEG1430.0100 100 mg € 300,00

PEG1430.0001 1 g € 625,00

HO OO

OO

O

O

OH

O

4,7,10,13,16-Pentaoxanonadecane-1,19-dioic acid CAS-NO: FORMULA: C

14H

26O

9

MOLECULAR WEIGHT: 338,35 g/moleFURTHER INFORMATION: Spacer is 19atoms and 21.7 A


PEG1435.0001 1 g € 725,00

NO O

OO

OO O

ON

O

OOO

O

Bis-succinimidyl-4,7,10,13,16-pentaoxanonadecane-1,19-dioate CAS-NO: FORMULA: C

22H

32N

2O

13



PEG4050.1000 1 g € 700,00O

O OO

4

O

O

F

F

F

F

F

F

F

F

F

F

alpha,omega-Bis(pentafluorphenyl propionate) tetra(ethylene glycol) CAS-NO: FORMULA: C

26H

24F

10O

9


PEG2115 NHS-PEG(4)-CO-OBzl PEG2115.0100 100 mg € 375,00

PEG2115.0001 1 g € 1000,00

OO OO

O

OOO

O

N

O

O

alpha-succinimidyl ester-omega-carboxy benzyl ester tetra(ethylene glycol) CAS-NO: FORMULA: C

25H

35NO

11


PEG1450 HOOC-dPEG™(6)-COOH PEG1450.0100 100 mg € 425,00

PEG1450.0001 1 g € 800,00HO O

O OH

O

O6

4,7,10,13,16,19,22-Heptaoxapentaeicosane-1,25-dioic acid CAS-NO: FORMULA: C

18H

34O

11



PEG3970.1000 1 g € 950,00O

O OO

N6

O

O

NO

O

O

O

Bis-succinimidyl-4,7,10,13,16,19,22-heptaoxa pentacosane-1,25-dioate CAS-NO: FORMULA: C

26H

40N

2O

15







PEG4060.1000 1 g € 950,00O

O OO

6

O

O

F

F

F

F

F

F

F

F

F

F

alpha,omega-Bis(pentafluorphenyl propionate) hexa(ethylene glycol) CAS-NO: FORMULA: C

30H

32F

10O

11



PEG1475.0001 1 g € 1000,00

HO OO OH

O

O8

4,7,10,13,16,19,22,25,28-Nonaoxauntriacontane-1,31-dioic acid CAS-NO: FORMULA: C

22H

42O

13

MOLECULAR WEIGHT: 514,56 g/moleFURTHER INFORMATION: Spacer os 31 atoms and 35.7 A

PEG1460 NHS-dPEG™(8)-NHS PEG1460.0001 1 g € 1000,00

O OO O

O

O8N

N

O

O

O

O

Bis-succinimidyl-4,7,10,13,16,19,22,25,28-nonaoxahentriacontane-1,31-dioate CAS-NO: FORMULA: C

30H

48N

2O

17



PEG4070.1000 1 g € 1150,00O

O OO

8

O

O

F

F

F

F

F

F

F

F

F

F

alpha,omega-Bis(pentafluorphenyl propionate) octa(ethylene glycol) CAS-NO: FORMULA: C

34H

40F

10O

13


PEG1091 HOOC-PEG(12)-COOH PEG1091.0001 1 g € 200,00

PEG1091.0005 5 g € 675,00HO O

O OH

O

O12

alpha,omega-Bis(propionic acid) dodecae(ethylene glycol) CAS-NO: 892155-64-5 FORMULA: C

30H

58O

17



PEG3980.1000 1 g € 1250,00O

O OO

N12

O

O

NO

O

O

O

alpha,omega-bis(succinimidyl propionate) dodeca(ethylen glycol) CAS-NO: FORMULA: C

38H

64N

2O

21



PEG4080.1000 1 g € 1250,00O

O OO

12

O

O

F

F

F

F

F

F

F

F

F

F

alpha,omega-Bis(pentafluorphenyl propionate) dodeca(ethylene glycol) CAS-NO: FORMULA: C

42H

56F

10O

17



PEG4140.1000 1 g € 1250,00O

O OHHO

16

O

O

alpha,omega-Bis(propionic acid) hexadeca(ethylene glycol) CAS-NO: FORMULA: C

38H

74O

21



PEG3990.1000 1 g € 1350,00O

O OO

N16

O

O

NO

O

O

O

alpha,omega-bis(succinimidyl propionate) hexadeca(ethylen glycol) CAS-NO: FORMULA: C

46H

80N

2O

25







PEG4090.1000 1 g € 1350,00O

O OO

16

O

O

F

F

F

F

F

F

F

F

F

F

alpha,omega-Bis(pentafluorphenyl propionate) hexadeca(ethylene glycol) CAS-NO: FORMULA: C

50H

72F

10O

21



PEG4150.1000 1 g € 1350,00O

O OHHO

20

O

O

alpha,omega-Bis(propionic acid) 20(ethylene glycol) CAS-NO: FORMULA: C

46H

90O

25



PEG4000.1000 1 g € 1400,00O

O OO

N20

O

O

NO

O

O

O

alpha,omega-bis(succinimidyl propionate) 20(ethylen glycol) CAS-NO: FORMULA: C

54H

96N

2O

29



PEG4100.1000 1 g € 1400,00O

O OO

20

O

O

F

F

F

F

F

F

F

F

F

F

alpha,omega-Bis(pentafluorphenyl propionate) 20(ethylene glycol) CAS-NO: FORMULA: C

58H

88F

10O

25



PEG4160.1000 1 g € 1400,00O

O OHHO

24

O

O

alpha,omega-Bis(propionic acid) 24(ethylene glycol) CAS-NO: FORMULA: C

54H

106O

29



PEG4010.1000 1 g € 1450,00O

O OO

N24

O

O

NO

O

O

O

alpha,omega-bis(succinimidyl propionate) 24(ethylen glycol) CAS-NO: FORMULA: C

62H

112N

2O

33


PEG4110 Tfp-dPEG™(24)-Tfp PEG4110.0100 100 mg € 450,00

PEG4110.1000 1 g € 1450,00O

O OO

24

O

O

F

F

F

F

F

F

F

F

alpha,omega-Bis(2,3,4,5-tetrafluorphenyl propionate) 24(ethylene glycol) CAS-NO: FORMULA: C

66H

106F

8O

29



PEG1465.1000 1 g € 1600,00HO O

O OH

O

O28

alpha,omega-Bis-carboxy-28(ethylen glycol) CAS-NO: FORMULA: C

60H

118O

32


PEG1189 tBu-O2C-PEG(12)-COOH PEG1189.0001 1 g € 250,00

PEG1189.0005 5 g € 1000,00

PEG1189.0025 25 g € 4000,00O

HN

NH

O NH

OH

O

O

O

O312

Oalpha-Alanine-t-butyl ester omega carboxylic acid PEG-dodecamer (3869 Dalton) CAS-NO: FORMULA: C

179H

331N

25O

65






PEG1083 HOOC-PEG-COOH PEG1083.0001 1 g € 75,00

PEG1083.0005 5 g € 275,00

NH

ONH

n

OH

O

OO

HO

O

alpha,omega-Bis-carboxy poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1085.0005 5 g € 275,00NH

ONH

n

OH

O

OO

HO

O



PEG1086.0005 5 g € 275,00

NH

ONH

n

OH

O

OO

HO

O



PEG1082.0005 5 g € 275,00NH

ONH

n

OH

O

OO

HO

O



PEG1084.0005 5 g € 275,00NH

ONH

n

OH

O

OO

HO

O


PEG1184 NHS-PEG-NHS PEG1184.0001 1 g € 165,00

PEG1184.0005 5 g € 560,00NH

ONH

n

O

O

OO

O

O

N N

O

O O

O

alpha,omega-Di-succinimidyl ester poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1186.0005 5 g € 560,00NH

ONH

n

O

O

OO

O

O

N N

O

O O

O



PEG1187.0005 5 g € 560,00NH

ONH

n

O

O

OO

O

O

N N

O

O O

O



PEG1183.0005 5 g € 560,00NH

ONH

n

O

O

OO

O

O

N N

O

O O

O



PEG1185.0005 5 g € 560,00NH

ONH

n

O

O

OO

O

O

N N

O

O O

O



NH

ONH

n

OH

O

OO

HO

O

NH

ONH

n

O

O

OO

O

O

N N

O

O O

O





3.3.6 mPeG- and other Alkyl-PeG-Acids, esters and carbamates

Carbonates are a convenient alternative to NHS ester reacting with amines and resulting in carbamates, which are stable under most conditions, but will hydrolyse at reduced pH.

PEG2020 DOHA PEG2020.0005 5 g € 200,00

PEG2020.0025 25 g € 600,00

PEG2020.0100 100 g € 1800,00O

OOH

O3,6-Dioxaheptanoic acid CAS-NO: 16024-56-9 FORMULA: C

5H

10O

4


PEG2025 TODA PEG2025.0025 25 g € 90,00

PEG2025.0100 100 g € 290,00

OO

OH

O

O

3,6,9-Trioxadecanoic acid CAS-NO: 16024-58-1 FORMULA: C

7H

14O

5


PEG1203 Stea-O2Oc-OH PEG1203.0001 1 g € 175,00

PEG1203.0005 5 g € 650,00

PEG1203.0025 25 g € 2500,00

NH

OO

O

OH

O

8-(Stearoylamido)-3,6-dioxaoctanoic acid CAS-NO: FORMULA: C

24H

47NO

5


PEG1630 MeO-EPr-COOH PEG1630.0100 100 mg € 250,00

PEG1630.0001 1 g € 600,00

OO OH

O3-(2-Methoxyethoxy)propanoic acid, 4,7-Dioxa-octanoic acid CAS-NO: FORMULA: C

6H

12O

4


PEG1905 MeO-EPr-NHS PEG1905.0100 100 mg € 300,00

PEG1905.0001 1 g € 600,00

OO O

O

N

O

O

3-(2-Methoxyethoxy)propanoic acid succinimidyl ester, 4,7-Dioxa-octanoic acid NHS ester CAS-NO: FORMULA: C

10H

15NO

6


PEG1620 MeO-dPEG™(3)-COOH PEG1620.0100 100 mg € 250,00

PEG1620.0001 1 g € 600,00O

OO

O OH

O2,5,8,11-Tetraoxatetradecan-14-oic acid CAS-NO: FORMULA: C

10H

20O

6


PEG1880 MeO-dPEG™(3)-NHS PEG1880.0100 100 mg € 300,00

PEG1880.0001 1 g € 600,00O

OO

O O

O

N

O

O

2,5,8,11-Tetraoxatetradecan-14-oic acid succinimidyl ester CAS-NO: FORMULA: C

14H

23NO

8


OMeO

OOn

O

N

O

O

NH2OMe

OON

H n

O

+

OMeO

OOn

O

N

O

O

NH2OMe

OON

H n

O

+




PEG1680 MeO-dPEG™(3)-O-CO-NHS PEG1680.0100 100 mg € 300,00

PEG1680.0001 1 g € 600,00

OO

OO O

N

OO

O

2-(2-(2-methoxyethoxy)ethoxy)ethyl succinimidyl carbonate CAS-NO: FORMULA: C

12H

19NO

8



PEG3380.1000 1 g € 700,00

MeO

OO

6

ON

OO

O

alpha-Methoxy-omega-succinimidyl carbonate hepta(ethylene glycol) CAS-NO: FORMULA: C

20H

35NO

12



PEG1625.0001 1 g € 650,00MeO

O OH

O7

2,5,8,11,14,17,20,23-Octaoxahexacosan-26-oic acid CAS-NO: FORMULA: C

18H

36O

10

MOLECULAR WEIGHT: 412,47 FURTHER INFORMATION: spacer is 26 atoms and 29.8 A


PEG1885.0001 1 g € 700,00MeO

O ON

O

OO

7

2,5,8,11,14,17,20,23-Octaoxahexacosan-26-oic acid succinimidyl ester CAS-NO: 756525-90-3 FORMULA: C

22H

39NO

12



PEG1645.0001 1 g € 850,00Me

OO

O

10

ON

OO

O

2,5,8,11,14,17,20,23,26,29,32-undecaoxatetratriacontan-34-yl succinimidyl carbonate CAS-NO: FORMULA: C

28H

51NO

16


PEG1156 MeO-PEG(12)-COOH PEG1156.0001 1 g € 375,00

PEG1156.0005 5 g € 1200,00MeO

O OH

O

11

alpha-Methoxy-omega-propionic acid undecae(ethylene glycol), 2,5,8,11,14,17,20,23,26,29,32,35-Dodecaoxaoctatriacontan-38-oic acid CAS-NO: FORMULA: C

26H

52O

14



PEG1890.0001 1 g € 650,00MeO

O O

O11N

O

O

2,5,8,11,14,17,20,23,26,29,32,35-Dodecaoxaoctatriacontan-38-oic acid succinimidyl ester CAS-NO: FORMULA: C

30H

55NO

16



PEG3390.1000 1 g € 1000,00Me

OO

O

14

ON

OO

O

alpha-Methoxy-omega-succinimidyl carbonate pentadeca(ethylene glycol) CAS-NO: FORMULA: C

36H

67NO

20


PEG2370 MeO-PEG(16)-COOH PEG2370.0100 100 mg € 300,00

PEG2370.0001 1 g € 775,00O

OMeO14

OH

Oalpha-Methoxy-omega-carboxy hexadeca(ethylene glycol) CAS-NO: FORMULA: C

34H

68O

18








PEG1895.0001 1 g € 775,00Me

OO O

O15N

O

O

alpha-Methoxy-15(ethylen glycol)-omega-propionic acid succinimidyl ester CAS-NO: FORMULA: C

38H

71NO

20



PEG3400.1000 1 g € 1100,00

MeO

OO

18

ON

OO

O

alpha-Methoxy-omega-succinimidyl carbonate nonadeca(ethylene glycol) CAS-NO: FORMULA: C

44H

83NO

24



PEG3410.1000 1 g € 1250,00

MeO

OO

22

ON

OO

O

alpha-Methoxy-omega-succinimidyl carbonate 23(ethylene glycol) CAS-NO: FORMULA: C

52H

99NO

28



PEG1635.0001 1 g € 1150,00

MeOO OH

O23

alpha-Methoxy-23(ethylen glycol)-omega-propionic acid, 4,7,10,13,16,19,22,25,28,31,34,37,40,43,46,49,52,55,58,61,64,67,70,73-tetra-cosaoxatertaheptacontanoic acid CAS-NO: FORMULA: C

50H

100O

26


PEG1900 MeO-dPEG™(24)-NHS PEG1900.0001 1 g € 1150,00

PEG1900.0005 5 g € 4500,00MeO

O O

O23N

O

O


54H

103NO

28



PEG3210.1000 1 g € 1550,00MeO

O OH

O36

alpha-Methoxy-37(ethylen glycol)-omega-propionic acid CAS-NO: FORMULA: C

76H

152O

39

MOLECULAR WEIGHT: 1690 g/moleFURTHER INFORMATION: Spacer length 112 atoms or 133.9 A


PEG3190.1000 1 g € 1550,00MeO

O O

O36N

O

O


80H

155NO

41



PEG3220.1000 1 g € 2000,00MeO

O OH

O48

alpha-Methoxy-49(ethylen glycol)-omega-propionic acid CAS-NO: FORMULA: C

100H

200O

51



PEG3200.1000 1 g € 1750,00MeO

O O

O48N

O

O


104H

203NO

53





PEG1166 MeO-PEG-NHS PEG1166.0001 1 g € 225,00

PEG1166.0005 5 g € 725,00MeOO

NHn

O

O

O

N

O

O

alpha-Methoxy-omega-carboxylic acid succinimidyl ester poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 g/mole


PEG1163.0005 5 g € 575,00MeOO

NHn

O

O

O

N

O

O

alpha-Methoxy-omega-carboxylic acid succinimidyl ester poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1165.0005 5 g € 575,00

PEG1165.0025 25 g € 1950,00

MeOO

NHn

O

O

O

N

O

O

alpha-Methoxy-omega-carboxylic acid succinimidyl ester poly(ethylene glycol) (PEG-MW 5.000 Dalton) MOLECULAR WEIGHT: 5000 DaFURTHER INFORMATION: spacer is 44 atoms and 50.7 A


PEG1162.0005 5 g € 700,00MeOO

NHn

O

O

O

N

O

O



PEG1164.0005 5 g € 700,00MeOO

NHn

O

O

O

N

O

O


PEG1202 MeO-PEG-O-CO-NHS PEG1202.0500 500 mg € 1100,00

PEG1202.0001 1 g € 1400,00

PEG1202.0002 2 g € 2600,00

MeOO

O O

n O

N

O

O

alpha-Methoxy-omega-succinimidyl carbonate poly(ethylene glycol) (PEG-MW 20.000 Da) MOLECULAR WEIGHT: 20000 Da

PEG1161 MeO-PEG-COOH PEG1161.0001 1 g € 120,00

PEG1161.0005 5 g € 450,00alpha-Methoxy-omega-carboxylic acid poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 Da


PEG1158.0005 5 g € 275,00alpha-Methoxy-omega-carboxylic acid poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da







Other NHS-carbonate-PEG derivatives available on custom synthesis basis.

MeOO

NHn

O

OH

O

MeOO

NHn

O

O

O

N

O

O





3.3.7 Dye labeled PeG-AcidsDyes normally have an extended aromatic and therefore mostly hydrophobic ring system. The incorporation of PEG spacer furnishes this class of molecules with good water solubility.

Used for protein or peptide labeling via direct coupling to amino functions.

Protocol for in situ activation:Use a 10-20% molar excess of EDC and NHS in dry methylene chloride (dried over 3 A molecular sieves). Add a methy-lene chloride solution of the acid to the dry reagents under dry conditions. Stir for several hours or overnight. Then evaporate the solvent and use.

Alternatively the reaction mixture can be treated with silica gel to adsorb excess of EDC and urea. Filter, then evaporate the solvent and use.

The NHS should be added together with the EDC, in order to prevent formation of anhydrides.

Plenty of alternative methods work equally well, like activation with DSC (N,N’-disuccinimidyl carbonate) and TEA or carbodiimides other than EDC (e.g. DIC, DCC).

For more Dyes and Fluorescence labels from Violet to NIR visit our website

www.iris-biotech.de/life-sciences/dyes.html

PEG1545 Rhodamine B-dPEG™(4)-COOH PEG1545.0010 10 mg € 325,00

OO

OO

NH

O

OHSO

O

SO3-

ON N+

1-(Rhodamin B-sulfonamido)-3-oxo-7,10,13,16-tetraoxa-4-azanonadecan-19-oic acid CAS-NO: FORMULA: C

38H

51N

3O

12S

2


3.4 PeG-Amines, hydrazines, Guanidines3.4.1 Mono Protected PeG-diamines

BNN1017 Boc-EDA*HCl BNN1017.0005 5 g € 150,00

BNN1017.0025 25 g € 600,00

O NH

NH2

ON-t-Butyloxycarbonyl-ethylenediamine hydrochloride CAS-NO: 79513-35-2 FORMULA: C

7H

16N

2O

2*HCl


BNN1016 Boc-DOOA BNN1016.0001 1 g € 80,00

BNN1016.0005 5 g € 275,00

BNN1016.0025 25 g € 1100,00O NH

OO

NH2

O1-(t-Butyloxycarbonyl-amino)-3,6-dioxa-8-octaneamine, liq. CAS-NO: 153086-78-3 FORMULA: C

11H

24N

2O

4


BNN1058 Boc-DSOA*HCl BNN1058.0001 1 g € 250,00

BNN1058.0005 5 g € 1000,00

O NH

SS

NH2

O1-(t-Butyloxycarbonyl-amino)-3,6-dithio-8-octaneamine hydrochloride CAS-NO: 1301739-93-4 FORMULA: C

11H

24N

2O

2S

2*HCl


BNN1015 Boc-DODA BNN1015.0001 1 g € 100,00

BNN1015.0005 5 g € 300,00

BNN1015.0025 25 g € 1200,00O NH

OO

O

NH2

1-(t-Butyloxycarbonyl-amino)-4,9-dioxa-12-dodecanamine, liq. CAS-NO: 275823-77-3 FORMULA: C

15H

32N

2O

4







PEG4660 Amino-dPEG™(11)-aminoxy-Boc PEG4660.0100 100 mg € 450,00

PEG4660.1000 1 g € 1275,00

11H2N

OO

HN O

O

alpha-Amino-omega-(t-butyloxycarbonyl-aminoxy)-undeca(ethylene glycol) CAS-NO: FORMULA: C

29H

60N

2O

14


PEG1068 Boc-NH-PEG-NH2 PEG1068.0500 500 mg € 175,00

PEG1068.0001 1 g € 275,00NH2O

HNO

O n

alpha-t-Butyloxycarbonylamino-omega-amino poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG1069.0001 1 g € 275,00NH2O

HNO

O n



PEG1067.0001 1 g € 325,00NH2O

HNO

O n


BNN1028 Boc-TOTA BNN1028.0001 1 g € 100,00

BNN1028.0005 5 g € 300,00

BNN1028.0025 25 g € 1200,00

O NH

OO

O

O NH2

1-(t-Butyloxycarbonyl-amino)-4,7,10-trioxa-13-tridecanamine, liq. CAS-NO: 194920-62-2 FORMULA: C

15H

32N

2O

5

MOLECULAR WEIGHT: 320,43 g/moleFURTHER INFORMATION: Spacer is 15 atoms amd 16.9 A

PEG1066 Boc-NH-PEG(8)-NH2 PEG1066.0001 1 g € 490,00

PEG1066.0005 5 g € 1650,00NH2O

HNO

O 7

alpha-Amino-omega-Boc-amino-octa(ethylene glycol) CAS-NO: 206265-98-7 FORMULA: C

21H

44N

2O

9


PEG1065 Boc-NH-PEG(12)-NH2 PEG1065.0001 1 g € 490,00

PEG1065.0005 5 g € 1650,00NH2O

HNO

O 11

alpha-Amino-omega-Boc-amino-dodecae(ethylene glycol) CAS-NO: 890091-42-6 FORMULA: C

29H

60N

2O

13


This bis-carbonly reactive PEG crosslinker can be used to conjugate two different aldehyde containing targets.

Aldehyde functions are present in carbohydrates, carbo-hydrate containing proteins and in oxidizable matrices.

Amino functions, however, can also be converted to aldehydes with formyl-PEG-active esters or simply with glutar-dialdehyde.


NH2O

HNO

O n




PEG1805 Fmoc-NH-dPEG™(4)-NHNH-Boc PEG1805.0100 100 mg € 300,00

PEG1805.0001 1 g € 800,00

OO

OO

HN

O

HN

O

ONH

O

O

15-(9-Fluorenyloxycarbonyl)amino-4,7,10,13-tetraoxa-pentadecanoyl-N‘-(t-butyloxycarbonyl)hydrazid CAS-NO: FORMULA: C

31H

43N

3O

9


FNN1008 Fmoc-EDA*HCl FNN1008.0005 5 g € 175,00

FNN1008.0025 25 g € 700,00O N

H

NH2

ON

1-(9-Fluorenylmethyloxycarbonyl)-ethylenediamine hydrochloride

CAS-NO: 166410-32-8 FORMULA: C17H

18N

2O

2*HCl


FNN1007 Fmoc-DOOA*HCl FNN1007.0001 1 g € 100,00

FNN1007.0005 5 g € 350,00

FNN1007.0025 25 g € 1400,00O N

HO

ONH2

O1-(9-Fluorenylmethyloxycarbonyl-amino)-3,6-dioxa-8-octaneamine hydrochloride CAS-NO: 868599-73-9 FORMULA: C

21H

26N

2O

4*HCl


FNN1006 Fmoc-DODA*HCl FNN1006.0001 1 g € 110,00

FNN1006.0005 5 g € 375,00

FNN1006.0025 25 g € 1500,00O N

HO

O

O

NH2

1-(9-Fluorenylmethyloxycarbonyl-amino)-4,9-dioxa-12-dodecaneamine hydrochloride CAS-NO: FORMULA: C

25H

34N

2O

4*HCl


FNN1011 Fmoc-TOTA*HCl FNN1011.0001 1 g € 110,00

FNN1011.0005 5 g € 375,00

FNN1011.0025 25 g € 1500,00O N

HO

O

O

O NH2

1-(9-Fluorenylmethyloxycarbonyl-amino)-4,7,10-trioxa-13-tridecanamine hydrochloride CAS-NO: 868599-75-1 FORMULA: C

25H

34N

2O

5*HCl


PEG1335 H2N-dPEG™(4)-NHNH-BocPEG1335.0100 100 mg € 300,00

PEG1335.0001 1 g € 775,00O

OO

OH2N

O

HN

NH

O

O15-Amino-4,7,10,13-tetraoxa-pentadecanoyl-N‘-(t-butyloxycarbonyl)-hy-drazid CAS-NO: FORMULA: C

16H

33N

3O

7


PEG4230 H2N-dPEG™(8)-NHNH-Boc PEG4230.0100 100 mg € 375,00

PEG4230.1000 1 g € 1000,00O

H2N

O

HN

NH

O

O

8

alpha-Amino-omega-(N‘-(t-butyloxycarbonyl)hydrazido propionate) octa(ethylene glycol) CAS-NO: FORMULA: C

24H

49N

3O

11

MOLECULAR WEIGHT: 555,66 g/moleFURTHER INFORMATION: Spacer are 30 atoms and 35.9 A approx

PEG4240 H2N-dPEG™(12)-NHNH-Boc PEG4240.0100 100 mg € 425,00

PEG4240.1000 1 g € 1100,00O

H2N

O

HN

NH

O

O

12

alpha-Amino-omega-(N‘-(t-butyloxycarbonyl)hydrazido propionate) dodeca(ethylene glycol) CAS-NO: FORMULA: C

32H

65N

3O

15



The amine terminus can react with either an acid/active ester or a carbonyl (aldehyde or ketone). The hydrazide (after Boc removal) can react with carboxyl or carbonyl moieties (aldehyde/ketone). The Boc group is being removed with TFA (25% TFA in DCM, 0°C or neat RT, 10 min).

The hydrazone formed from the incipient hydrazide can be used as a cleavable linking site, as the hydrazone is stable at pH above 7, and can be cleaved under acid pH.

The hydrazone can then be used as a release point in a delivery system, for example. The Boc protected hydrazide is not particularly water soluble, but is very soluble in most organic solvents, however, its inherent hydrophilicity is high once incorporated as a conjugated system.

When incorporated the spacer will increase water solubil-ity and reduce aggregation while remaining nonimmuno-genic and non-toxic.

Orthogonal bis-carbonyl/carboxyl reactive PEGylating reagent.




Z-protected amino-PEG-acids typically are applied in solu-tion synthesis for incorporating a PEG unit using standard Cbz-chemistry, either as a spacer or terminal group in peptide sequences, typically applied in solution synthesis.

The Cbz or Z protecting group is being deprotected by hydrogenolysis using catalytic Pd/C.

PEG spacer provide water solubility, reduce or eliminate aggregation, and are inherently non-immunogenic and non-toxic.

PEG1745 Z-NH-dPEG™(3)-NH2 PEG1745.0001 1 g € 480,00

OO

O NH2NH

O

O

3-(2-(2-(3-Benzyloxycarbonylaminopropoxy)ethoxy)ethoxy)propylamine CAS-NO: FORMULA: C

18H

30N

2O

5


3.4.2 Unprotected PeG-diamines

PEG1204 H2N-PEG(8)-NH2 PEG1204.0005 5 g € 500,00

OH2N NH2

7

alpha,omega-Bis-amino octa(ethylene glycol) CAS-NO: FORMULA: C

16H

36N

2O

7


PEG1500 H2N-dPEG™(11)-NH2 PEG1500.0100 100 mg € 300,00

PEG1500.0001 1 g € 800,00

OHNO

ONH

O4

O

O2

OO

2

H2NNH2

N1,N

19-bis(3-(2-(2-(3-aminopropoxy)ethoxy)ethoxy)propyl)-4,7,10,13,16-

pentaoxanonadecane-1,19-diamide CAS-NO: FORMULA: C

34H

70N

4O

13


PEG1000 H2N-PEG(20)-NH2 PEG1000.0001 1 g € 250,00

PEG1000.0005 5 g € 750,00OH2N NH2

19

alpha,omega-Bis-amino 20(ethylene glycol) CAS-NO: 892154-56-2 FORMULA: C

40H

84N

2O

19


PEG1002 H2N-PEG-NH2 PEG1002.0001 1 g € 75,00

PEG1002.0005 5 g € 275,00NH2O

OH2N

n

alpha,omega-Bis-amino poly(ethylene glycol) (PEG-MW 2.000 Dalton) CAS-NO: 24991-53-5 FORMULA: - MOLECULAR WEIGHT: 2000 Da

PEG1004 H2N-PEG-NH2 PEG1004.0001 1 g € 75,00

PEG1004.0005 5 g € 275,00alpha,omega-Bis-amino poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: 24991-53-5 FORMULA: - MOLECULAR WEIGHT: 3000 Da

PEG1005 H2N-PEG-NH2 PEG1005.0001 1 g € 75,00


PEG1001 H2N-PEG-NH2 PEG1001.0001 1 g € 75,00


PEG1003 H2N-PEG-NH2 PEG1003.0001 1 g € 75,00



NH2O

OH2N

n




3.4.3 Amino-PeG-alcoholsBAL1048 Boc,Pbf-amidino-EtOH BAL1048.0001 1 g € 75,00

BAL1048.0005 5 g € 300,00

BAL1048.0025 25 g € 1200,00NOH

NH

HN

S

OO

O

O O2-(Boc,Pbf-amidino)ethanol, 2-[N-t-Butyloxycarbonyl-N‘-(2,2,4,6,7-pen-tamethyldihydrobenzofuran-5-sulfonyl)amidino]ethanol CAS-NO: 1263048-99-2 FORMULA: C

21H

33N

3O

6S


BAL1047 Boc,Pbf-amidino-EEtOH BAL1047.0001 1 g € 75,00

BAL1047.0005 5 g € 300,00

BAL1047.0025 25 g € 1200,00NO

NH

HN

S

OO

O

O O

OH

2-[2-(Boc,Pbf-amidino)ethoxy]ethanol, 2-{2-[N-t-Butyloxycarbonyl-N‘-(2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl)amidino]ethoxy}ethanol CAS-NO: 1263049-12-2 FORMULA: C

23H

37N

3O

7S


PEG1915 Boc-NH-dPEG™(4)-OH PEG1915.0100 100 mg € 300,00

PEG1915.0001 1 g € 600,00OH

OO

O

HNO

O

2-(2-(2-(2-(t-Butyloxycarbonylamino)ethoxy)ethoxy)ethoxy)ethanol CAS-NO: FORMULA: C

13H

27NO

6


PEG1960 Boc-NH-dPEG™(12)-OH PEG1960.0100 100 mg € 375,00

PEG1960.0001 1 g € 850,00O

HN

OOH

O 11

35-(t-Butyloxycarbonylamino)-3,6,9,12,15,18,21,24,27,30,33-un-decaoxapentatriacontan-1-ol CAS-NO: FORMULA: C

29H

59NO

14


PEG1021 Boc-NH-PEG-OH PEG1021.0500 500 mg € 175,00

PEG1021.0001 1 g € 290,00alpha-t-Butyloxycarbonylamino-omega-hydroxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da





PEG1030 HO-PEG-CONH-NH-Boc PEG1030.0500 500 mg € 230,00

PEG1030.0001 1 g € 380,00HO

ONH

HN

NH

O

O

O

O

n

alpha-Hydroxy-omega-t-butyloxycarbonyl-hydrazido poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG1031.0001 1 g € 380,00HOO

NH

HN

NH

O

O

O

O

n



PEG1029.0001 1 g € 430,00HO

ONH

HN

NH

O

O

O

O

n



OHO

NH n

O

O

HOO

NH

HN

NH

O

O

O

O

n




FAL3010 Fmoc-O1Pen-ol FAL3010.0005 5 g € 125,00

FAL3010.0025 25 g € 500,00NH

OOH

O

O5-(9-Fluorenylmethyloxycarbonyl-amino)-3-oxa-1-pentanol CAS-NO: 560088-66-6 FORMULA: C

19H

21NO

4


FAA6580 Fmoc-O2Oc-NH-CH2-CH(OMe)2 FAA6580.0000 Please inquire!

NHO

O

HN

O

O

O OMe

OMe1,1-Dimethoxy-11-[(9-Fluorenylmethyloxycarbonyl)amino]-4-oxo-6,9-

trioxa-3-azaundecan CAS-NO: FORMULA: C

25H

32N

2O

7


PEG1320 H2N-dPEG™(4)-OH PEG1320.0100 100 mg € 300,00

PEG1320.0001 1 g € 600,00OH

OO

OH2N

2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethanol CAS-NO: 86770-74-3 FORMULA: C

8H

19NO

4



PEG1340.0001 1 g € 700,00OHO

H2N

7

23-Amino-3,6,9,12,15,18,21-heptaoxatrieicosane-1-ol CAS-NO: FORMULA: C

16H

35NO

8



PEG1310.0001 1 g € 850,00H2NO

OH

11

35-Amino-3,6,9,12,15,18,21,24,27,30,33-undecaoxapentatriacontan-1-ol CAS-NO: FORMULA: C

24H

51NO

12


PEG1315 H2N-dPEG™(12)-O-DMT PEG1315.0100 100 mg € 375,00

PEG1315.0001 1 g € 850,00

H2NO

O

11

OMe

OMe

35-Amino-3,6,9,12,15,18,21,24,27,30,33-undecaoxapentatria-contan-1-(4,4‘-dimethoxytrityl)ether CAS-NO: FORMULA: C

45H

69NO

14



PEG3740.1000 1 g € 1150,00

H2NO

OH

23alpha-Amino-omega-hydroxy 24(ethylene glycol) CAS-NO: FORMULA: C

48H

99NO

24

MOLECULAR WEIGHT: 1074,29 g/moleFURTHER INFORMATION: Spacers are 71 atoms or 86.0 A


PEG3750.1000 1 g € 1450,00H2NO

OH

35

alpha-Amino-omega-hydroxy 36(ethylene glycol) CAS-NO: FORMULA: C

72H

147NO

36

MOLECULAR WEIGHT: 1602,92 g/moleFURTHER INFORMATION: Spacers are 107 atoms or 129.0 A


Carbonyl and carboxyl reactive PEGylating reagent that reacts with acids, active esters and aldehydes/ketones. The DMT (4,4’-dimethoxytrityl) protected hydroxyl func-

tion can be deprotected with mild acid, including TFE (triflouroethanol).




PEG1007 H2N-PEG-OH PEG1007.0500 500 mg € 135,00

PEG1007.0001 1 g € 225,00NH2O

OHO

n

alpha-Amino-omega-hydroxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) CAS-NO: 32130-27-1MOLECULAR WEIGHT: 3000 Da


PEG1008.0001 1 g € 275,00NH2O

OHO

n

alpha-Amino-omega-hydroxy poly(ethylene glycol) (PEG-MW 5.000 Dalton) CAS-NO: 32130-27-1 MOLECULAR WEIGHT: 5000 Da


PEG1006.0001 1 g € 275,00NH2O

OHO

n

alpha-Amino-omega-hydroxy poly(ethylene glycol) (PEG-MW 10.000 Dalton) CAS-NO: 32130-27-1 MOLECULAR WEIGHT: 10000 Da

Methoxy-PEG-amines react with carboxyl (acids/active es-ters) and carbonyl groups (aldehydes/ketones) to increase water solubility and decrease aggregation. They can be used for modification of surfaces to eliminate hydropho-bic interactions and, in combination with amino-PEG-acids, to cap with functionality. Potentially very useful as drug modifier to increase hydrodynamic volume.

Imparts significant water solubility, non-immunogenicity and non-toxicity. Soluble in all organic solvents from moderate to higher polarity (preferably DCM or DMAC).

Activation of the corresponding acid can be done with EDC and NHS. This is best done in a non-amine contain-ing buffer, e.g., in MES buffer at pH 5-6. Then raise the pH to 7.2 to 7.5 with phosphate buffer just before reacting with the amine or after the amine has been added.

General guidelines for use:In all cases care should be taken in handling amines. They are very hygroscopic and will react with atmosphere over time adsorbing water and carbondioxide (CO

2). Ap-

proriated handling and storage under inert atmosphere is required. Up to PEG(12) they are liquids, longer derivatives are solids, when kept cold.

Reference:



10: 0-12-370501-0). pp. 25, 215-233, and 726-729.

3.4.4 mPeG-amines

Reference:



10: 0-12-370501-0). pp. 215-233.


HN

O

O

O

O

O

HOO

HN

O

O

O

O

O

HN

O

O

O

O

O

HOO

HN

O

O

O

O

O

HN

O

O

O

O

O

HO

O

HN

O

O

O

O

O

HN

O

O

O

O

O

HN

O

O

O

O

O

HO

O

HN

O

O

O

O

O

HN

O

O

O

O

O

HO

O

HN

O

O

O

O

O

HN

O

O

O

O

O

OH

O

HN

O

O

O

O

O

HO O

NH2O

OHO

n




PEG1685 MeO-dPEG™(4)-NH2 PEG1685.0100 100 mg € 275,00

PEG1685.0001 1 g € 700,00

MeO

OO

ONH2

2,5,8,11-Tetraoxatridecan-13-amine CAS-NO: FORMULA: C

9H

21NO

4


PEG1730 MeO-PEG(7)-NH2 PEG1730.0001 1 g € 285,00

MeO

ONH2

6

alpha-Methoxy-omega-amino hepta(ethylene glycol), 2,5,8,11,14,17,20-heptaoxadocosan-22-amine CAS-NO: FORMULA: C

15H

33NO

7



PEG1700.0001 1 g € 800,00Me

OO

NH2

7

2,5,8,11,14,17,20,23-Octaoxapentacosan-25-amine CAS-NO: FORMULA: C

17H

37NO

8



PEG1655.0001 1 g € 850,00MeOO

NH2

11

2,5,8,11,14,17,20,23,26,29,32,35-Dodecaoxaheptatriacontan-37-amine CAS-NO: FORMULA: C

25H

53NO

12



PEG3290.1000 1 g € 1100,00MeOO

NH2

14

alpha-Methoxy-omega-amino-15(ethylen glycol) CAS-NO: FORMULA: C

31H

65NO

15



PEG1670.0001 1 g € 1050,00MeOO

NH2

23


49H

101NO

24



PEG3300.1000 1 g € 1300,00MeOO

NH2

35


73H

149NO

36



PEG3310.1000 1 g € 1400,00MeOO

NH2

47


97H

197NO

48







PEG1155 MeO-PEG-NH2 PEG1155.0001 1 g € 90,00

PEG1155.0005 5 g € 350,00NH2O

OMeO

n

alpha-Methoxy-omega-amino poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 Da


PEG1152.0005 5 g € 275,00NH2O

OMeO

n

alpha-Methoxy-omega-amino poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1154.0005 5 g € 275,00NH2O

OMeO

n



PEG1151.0005 5 g € 350,00NH2O

OMeO

n



PEG1153.0005 5 g € 350,00NH2O

OMeO

n



NH2O

OMeO

n

Second generation dendrimer based on a pentavalent PEG based building block for sophisticated applications in

drug delivery, diagnostics, combination therapy or person-alized medicine.

PeG based Dendrimers – New hapten carrier Molecules




3.5 PeG-Alkynes&Azides for click-chemistrythe click Reaction

Azido and Alkyne functions can cyclize by an intramolecu-lar Cui or Cu0 catalyzed azide-alkyne 1,3-dipolar cycload-dition (CuAAC). This so-called Click Reaction, developed by K. Barry Sharpless and Morton Meldal, has meanwhile developed to a widely used type of reaction orthogonal to many other types of reactions in different kinds of applica-tions. Both residues R1 and R2 can be used either as con-jugation partner or as substrates. Due to its high thermo-dynamic driving force, usually greater than 20 kcal/mol, the click reaction normally proceeds rapidly to completion and also tends to be highly selective for a single product.

A variety of Azido and Alkyne Building Blocks is available,

where some can be incorporated into biomolecules by re-combinant syntheses, in particular by non natural protein translation using the amber-suppression-based orthogonal system or by chemical reactions, for example by solid phase synthesis. Then the conjugation with a second mol-ecule carrying the appropriate other function can be done.

f A stepwise Huisegen cycloaddition process: copper (I)-catalyzed

regioselective ligation of azides and terminal alkynes; V.V. Rostovt-

sev, L.G. Green, K.B. Sharpless; Angew. Chem. Int. Ed. 2002; 41: 2596-2599.

f C.W. Tornøe, C. Christensen; M. Meldal; Peptidotriazoles on solid

phase: [1,2,3]-triazoles by regiospecific copper(I)-catalyzed 1,3-dipo-

lar cycloaddition of terminal alkynes to azides; J.Org.Chem. 2002;

67: 3057-3064.

f Click Chemistry: Diverse Chemical Function from a Few Good Reac-

tions; H. C. Kolb, M. G. Finn, and K. Barry Sharpless, Angew. Chem.,

Int. Eng. Ed. 2001; 40: 2004-2021.

f The growing impact of click chemistry on drug discovery; H. C. Kolb

and K. Barry Sharpless; Drug Discovery Today 2003; 8(24): 1128-1131.

f Cu-Catalyzed Alkyne-Azide „Click“ Cycloadditions from a Mechanis-

tic and Synthetic Perspective; V. C. Bock, H. Hiemstra and J. H. van

Maarseveen; Eur. J. Org. Chem. 2006; 51-68.

f A3-Type Star Polymer via Click Chemistry; O. Altintas, B. Yankul, G.

Hizal and U. Tunca; J. Poly. Sci.: Part A, Polymer Chem. 2006; 44: 6458-6465.

f Preparation of alumina supported copper nanoparticles and their

application in the synthesis of 1,2,3- triazoles; M. L. Kantam, et al.; J.

Mol. Catal. A: Chem. 2006; 256: 273-277.

f A Rapid and Versatile Method to Label Receptor Ligand Using

„Click“ Chemistry: Validation with the Muscarinic M1 Antagonist

Pirenzepine; Bioconjugate Chemistry 2006; 17: 1618-1623.

f Alkyne-azide click reaction catalyzed by metallic copper under ul-

trasound; Pedro Cintas1, Alessandro Barge, Silvia Tagliapietra, Luisa

Boffa & Giancarlo Cravotto; Nature Protocols 2010; 5(3): 607-616.

f Synthesis of a DOTA-Biotin Conjugate for Radionuclide Chelation

via Cu-Free Click Chemistry; Michael K. Schultz, Sharavathi G.

Parameswarappa, and F. Christopher Pigge; Org. Lett. 2010; 12(10): 2398-2401.

References:




3.5.1 PeG-Alkynes PEG1935 Propargyl-NHS PEG1935.0100 100 mg € 300,00

PEG1935.0001 1 g € 550,00O ON

O

O

O

3-(Prop-2-ynyloxy)propanoic acid succinimidyl ester FORMULA: C

10H

11NO

5


PEG2755 Propargyl amine PEG2755.0001 1 g € 275,00

NH2

Propargyl amine CAS-NO: 2450-71-7 FORMULA: C

3H

5N


PEG2840 MeO-PEG-alkyne PEG2840.0500 500 mg € 230,00

PEG2840.0001 1 g € 400,00ONH

MeOn

Oalpha-Methoxy-omega-propargylacetamido poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 g/mole


PEG2810.0001 1 g € 200,00ONH

MeOn

Oalpha-Methoxy-omega-propargylacetamido poly(ethylene glycol) (PEG-MW 2000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG2830.0001 1 g € 200,00ONH

MeOn



PEG2800.0001 1 g € 225,00O

NH

MeOn



PEG2820.0001 1 g € 225,00ONH

MeOn

O

alpha-Methoxy-omega-propargylacetamido poly(ethylene glycol) (PEG-MW 20000 Dalton) MOLECULAR WEIGHT: 20000 Da


ONH

MeOn

O

In conjugation techniques with thiol groups from Cystein or other SH carrying moieties normally maleinimides are used which react also with other acid protons like for example from OH or NH

2 and give appropriate unwanted

impurities. The Iodo group reacts much more specifically with thiol resulting in much cleaner conjugates.

Reference:

f Quantitative reactivity profiling predicts functional cysteins in

proteomes K.Weerapana C.Wang G.M.Simon F.Richter S.Khare

M.B.D.Dillon D.A.Bachovichin K.Mowen D.Baker B.J.Cravatt Nature

2010; 468: 790-795.

+ I PEGR SH S PEGR




PEG3110 I-PEG-alkyne PEG3110.0100 100 mg € 225,00

PEG3110.0500 500 mg € 625,00alpha-Iodo-omega-propargylacetamido poly(ethylene glycol) (PEG-MW 3000 Dalton) MOLECULAR WEIGHT: 3000 Da








ONH

NH n

I

O O


2 and give appropri-

ate unwanted impurities. The Iodo group reacts much more specifically with thiol resulting in much cleaner conjugates.

Reference:




2010; 468: 790-795.

PEG2960 H2N-PEG-alkyne PEG2960.0500 500 mg € 370,00

PEG2960.0001 1 g € 610,00O

NH

H2Nn

Oalpha-Amino-omega-propargylacetamido poly(ethylene glycol) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG2980.0001 1 g € 610,00O

NH

H2Nn



PEG2950.0001 1 g € 675,00O

NH

H2Nn



PEG2970.0001 1 g € 675,00O

NH

H2Nn


ONH

H2Nn

O




PEG2860 NHS-PEG-alkyne PEG2860.0500 500 mg € 475,00

PEG2860.0001 1 g € 825,00

ONHn

O

O

O

N

O

O

alpha-Succinimidyl ester-omega-propargylacetamido poly(ethylene glycol) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG2880.0001 1 g € 825,00

ONHn

O

O

O

N

O

O



PEG2850.0001 1 g € 880,00

ONHn

O

O

O

N

O

O



PEG2870.0001 1 g € 880,00

ONHn

O

O

O

N

O

O


ONHn

O

O

O

N

O

O


H2N (S)(S)OH

O

(R)(R)

OH

H2NOH

O

OH

H2NOH

O

OH

serine threonine 3-hydroxy-leucineHAA1650

Visit our website www.iris-biotech.de with over 5000 Products!

Amino Acid Analogues for Peptidomimetics and Medicinal Chemistry.




PEG2910 NHS-PEG(NH-Boc)-alkyne PEG2910.0500 500 mg € 500,00

PEG2910.0001 1 g € 880,00HN

NH

OO

O

n

O

O

N

O

O

O

O

alpha-Succinimidyl ester-omega-(N-t-Butyloxycarbonyl-L-propargyl-glycinyl) poly(ethylene glycol) MOLECULAR WEIGHT: 3000 Da


PEG2930.0001 1 g € 880,00HN

NH

OO

O

n

O

O

N

O

O

O

O



PEG2900.0001 1 g € 960,00HN

NH

OO

O

n

O

O

N

O

O

O

O



PEG2920.0001 1 g € 960,00HN

NH

OO

O

n

O

O

N

O

O

O

O



HN

NH

OO

O

n

O

O

N

O

O

O

O

Boc

HN

NH

OO

O

n

O

O

NHS

1. The NHS group can react with nucleophiles like amines or alcohols.

2. At the Boc-Amino position the free amino group (after removal of the Boc protecting group) can form a stable amide bond with activated esters.

3. Finally the Alkyne function is still free for the Click reaction with the third partner.

Two interacting partners - like protein and receptor – can be conjugated in this way, and the interaction monitored by attaching a dye, fluorophore, NMR or spin label for highly sophisticated experiments.

tri-functional PeG cross-Linker

Tri-functional PEG, carrying three orthogonal reactive groups:

NHS-PEG(NH-Boc)-alkyne

α-succinimidyl ester-ω-(N-t-butyloxycarbonyl-L-propargyl-glycinyl) poly(ethylene glycol)

Conjugation with

-NH2

-N3 -COOH




PEG4810 Alkyne-PEG-Si(OMe)3 PEG4810.0500 500 mg € 500,00

PEG4810.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3

OOalpha-Propargylacetamido-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG4815.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3



PEG4820.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3



PEG4825.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3



NH

ONH

NH

nSi(OMe)3

OO

OSi

O

O

O

O

NH

OSi

O

O

O

O

O

Si

O

O

O

O

NH

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

OSi

O

O

O

O

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

OSi

O

O

O

O

NH

HO

HOHO

HOHO HO HO

HO

HO

HO

HO

HO

HOHO

HOHO

HOHO

HOOH

HO

HO

HOHO HO

HO

O

O

OO

O

O

O

The broad variety of the Click reaction can be applied on surfaces using appropriate PEG-silanes, where silicate particles can be coated with.





3.5.2 PeG-AzidesThe azide can potentially be reacted with an acetylene moiety (Click reaction) or an arylphospinederivative, as part of several Staudinger ligation options (see references). It can also be used as a precursor to the amine function in which it can be transformed via reduction with P(Ph)

3.

References Staudinger Ligation:

f The Staudinger Ligation-A Gift to Chemical Biology; M. Köhn, R.

Breinbauer; Angew. Chem. Int. Ed. 2004; 43: 3106.

f Traceless Staudinger Ligation of Glycosyl Azides with Triaryl Phos-

phines: Stereoselective Synthesis of Glycosyl Amides; A. Bianchi, A.

Bernardi; J. Org. Chem. 2006; 71: 4565-4577.

f Reaction Mechanism and Kinetics of the Traceless Staudinger

Ligation; M. Soelner, B. L. Nilsson, R. T. Raines; J. Amer. Chem. Soc.

2006; 128(27): 8820-8828.

f E. Saxon, C. R. Bertozzi; Science 2000; 287: 2007-2010.

f E. Saxon, J. I. Armstrong, C. R. Bertozzi; Org. Lett. 2000; 2: 2141-2143.

f B. L.Nilsson, L. L. Kiessling, R. T. Raines; Org. Lett. 2000, 2: 1939-

1941.

The Staudinger Ligation

+PEG N3

P

O

OMe

Ph

Ph

P+

O

OMe

N-

Ph Ph

PEGpH 7.4

- N2

P

HN

O

Ph Ph

PEG

+ H2O

- MeOH

O



10: 0-12-370501-0). Pp. 722-726.

f Chemoselective Staudinger-Phosphite Reaction of Azides for the

Phosphorylation of Proteins; Remigiusz Serwa, Ina Wilkening, Gi-

useppe Del Signore, Michaela Mühlberg, Iris Claußnitzer, Christoph

Weise, Michael Gerrits, and Christian P. R. Hackenberger; Angew.

Chem. Int. Ed. 2009; 48: 8234-8239; DOI: 10.1002/anie.200902118.

f R. Kleineweischede, C. P. R. Hackenberger; Angew. Chem. Int. Ed.

2008; 47: 5984-5988.

The tremendous attraction to the azide functionality is its very low reactivity and high stability under most conditions. However, under very specific conditions, the azide is very reactive and highly selective.




PEG3060 H2N-PEG(3)-N3 PEG3060.0100 100 mg € 250,00

PEG3060.0001 1 g € 850,00O

N3OO

H2N

1-Amino-11-azido-3,6,9-trioxaundecane, 2-{2-[2-(2-Azidoethoxy)ethoxy]ethoxy}ethylamine, O-(2-Aminoethyl)-O’-(2-azidoethyl)diethylene glycol CAS-NO: 134179-38-7 FORMULA: C

8H

18N

4O

3


Reference:

f C.R. Bertozzi M.D. Bednarski J. Org. Chem. 1991; 56: 4326 A.W.

Schwabacher et al. J. Org. Chem. 1998; 63: 1727

PEG1087 H2N-PEG(7)-N3 PEG1087.0001 1 g € 275,00

PEG1087.0005 5 g € 975,00

PEG1087.0025 25 g € 3500,00O

ON3

H2N5

alpha-Amino-omega-azido hepta(ethylene glycol) CAS-NO: 957486-82-7 FORMULA: C

14H

30N

4O

6


PEG2350 H2N-PEG(8)-N3 PEG2350.0100 100 mg € 325,00

PEG2350.0001 1 g € 1000,00O

ON3

H2N6

alpha-Amino-omega-azido octa(ethylene glycol) FORMULA: C

16H

34N

4O

7


PEG3050 H2N-PEG(9)-N3 PEG3050.0001 1 g € 275,00

PEG3050.0005 5 g € 975,00O

ON3

H2N7

alpha-Amino-omega-azido nona(ethylene glycol) FORMULA: C

18H

38N

4O

8


PEG3040 H2N-PEG(11)-N3 PEG3040.0001 1 g € 325,00

PEG3040.0005 5 g € 1100,00O

ON3

H2N9

alpha-Amino-omega-azido undeca(ethylene glycol) FORMULA: C

22H

46N

4O

10


PEG1081 H2N-PEG(12)-N3 PEG1081.0001 1 g € 350,00

PEG1081.0005 5 g € 1200,00

PEG1081.0025 25 g € 4250,00O

ON3

H2N10

alpha-Amino-omega-azido dodecae(ethylene glycol) FORMULA: C

24H

50N

4O

11

MOLECULAR WEIGHT: 570,69 g/moleFURTHER INFORMATION: Spacers are 36 atoms and 44.2 A approx

PEG3070 H2N-PEG(23)-N3 PEG3070.0100 100 mg € 425,00

PEG3070.0001 1 g € 1300,00O

N3H2N23

alpha-Azido-omega-amino 23(ethylene glycol) FORMULA: C

48H

98N

4O

23


PEG3080 H2N-PEG(35)-N3 PEG3080.0100 100 mg € 450,00

PEG3080.0001 1 g € 1400,00O

N3H2N35

alpha-Azido-omega-amino 35(ethylene glycol) FORMULA: C

72H

146N

4O

35






PEG3010 H2N-PEG-N3 PEG3010.0500 500 mg € 370,00

PEG3010.0001 1 g € 610,00O

N3H2Nn

alpha-Amino-omega-azido poly(ethylene glycol) (PEG-MW 3000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -

PEG3030 H2N-PEG-N3 PEG3030.0500 500 mg € 370,00

PEG3030.0001 1 g € 610,00O

N3H2Nn

alpha-Amino-omega-azido poly(ethylene glycol) FORMULA: - MOLECULAR WEIGHT: 5000 DaFURTHER INFORMATION: -

PEG3000 H2N-PEG-N3 PEG3000.0500 500 mg € 400,00

PEG3000.0001 1 g € 675,00O

N3H2Nn


PEG3020 H2N-PEG-N3 PEG3020.0500 500 mg € 400,00

PEG3020.0001 1 g € 675,00O

N3H2Nn


PEG3760 N3-dPEG™(4)-OH PEG3760.0100 100 mg € 275,00

PEG3760.1000 1 g € 750,00

OO

ON3HO

alpha-Azido-omega-hydroxy tetra(ethylene glycol) FORMULA: C

8H

17N

3O

4


PEG1088 N3-PEG(8)-OH PEG1088.0001 1 g € 300,00

PEG1088.0005 5 g € 900,00O

OOH

N36

alpha-Azido-omega-hydroxy octa(ethylene glycol) FORMULA: C

16H

33N

3O

8

MOLECULAR WEIGHT: 395,45 g/moleFURTHER INFORMATION: spacers are 24 atoms and 29.5 A approx.


PEG1390.0001 1 g € 850,00O

OOH

N310

35-Azido-3,6,9,12,15,18,21,24,27,30,33-undecaoxapentatriacontan-1-ol FORMULA: C

24H

49N

3O

12


PEG1220 N3-PEG(20)-OH PEG1220.0001 1 g € 325,00

PEG1220.0005 5 g € 975,00O

OOH

N318

alpha-Azido-omega-hydroxy icosa(ethylene glycol) FORMULA: C

40H

81N

3O

20



ON3H2N

n





PEG3770.1000 1 g € 1000,00N3O

HO

23

alpha-Azido-omega-hydroxy 24(ethylene glycol) FORMULA: C

48H

97N

3O

24



PEG3780.1000 1 g € 1150,00N3O

HO

35

alpha-Azido-omega-hydroxy 36(ethylene glycol) FORMULA: C

72H

145N

3O

36


PEG1690 MeO-dPEG™(4)-N3 PEG1690.0100 100 mg € 275,00

PEG1690.0001 1 g € 700,00O

OO

ON3

13-Azido-2,5,8,11-tetraoxa-tridecane FORMULA: C

9H

19N

3O

4



PEG1705.0001 1 g € 800,00MeOO

N3

7

2,5,8,11,14,17,20,23-Octaoxapentacosan-25-amine FORMULA: C

17H

35N

3O

8



PEG1660.0001 1 g € 850,00MeOO

N3

11

37-Azido-2,5,8,11,14,17,20,23,26,29,32,35-dodecaoxaheptatriacontane FORMULA: C

25H

51N

3O

12



PEG1710.0001 1 g € 1000,00MeOO

N3

23

alpha-Methoxy-omega-azido-24(ethylene glycol) FORMULA: C

49H

99N

3O

24



PEG3430.1000 1 g € 1250,00MeOO

N3

35

alpha-Methoxy-omega-azido-36(ethylene glycol) FORMULA: C

73H

147N

3O

36







PEG1219 MeO-PEG-N3 PEG1219.0500 500 mg € 230,00

PEG1219.0001 1 g € 400,00O

ON3

MeOn

alpha-Methoxy-omega-azido poly(ethylene glycol) FORMULA: - MOLECULAR WEIGHT: 750 g/moleFURTHER INFORMATION: -


PEG1225.0001 1 g € 200,00O

ON3

MeOn

alpha-Methoxy-omega-azido poly(ethylene glycol) FORMULA: - MOLECULAR WEIGHT: 2000 DaFURTHER INFORMATION: -


PEG2040.0001 1 g € 200,00O

ON3

MeOn



PEG2045.0001 1 g € 225,00O

ON3

MeOn



PEG2050.0001 1 g € 225,00O

ON3

MeOn


PEG2780 N3-O2Oc-OH*CHA PEG2780.0001 1 g € 250,00

PEG2780.0005 5 g € 1000,00N

OO

OH

ON+

-N

8-Azido-3,6-dioxaoctanoic acid cyclohexylamine, 2-(2-Azidoethoxy)ethoxyacetic acid cyclohexylamine CAS-NO: 88518-90-3 net FORMULA: C

6H

11N

3O

4*C

6H

13N

MOLECULAR WEIGHT: 189.17*99.17 g/moleFURTHER INFORMATION: -

PEG2345 N3-PEG(4)-COOH PEG2345.0100 100 mg € 325,00

PEG2345.0001 1 g € 925,00

OO

N3O

O OH

O15-Azido-4,7,10,13-tetraoxa-pentadecanoic acid FORMULA: C

11H

21N

3O

6


PEG1400 N3-dPEG™(4)-NHS PEG1400.0100 100 mg € 300,00

PEG1400.0001 1 g € 1000,00O

OO

ON3

O

ON

O

O

15-Azido-4,7,10,13-tetraoxa-pentadecanoic acid succinimidyl ester FORMULA: C

15H

24N

4O

8



OO

N3MeO

n




PEG2790 N3-O2Oc-O2Oc-OH*CHA PEG2790.0001 1 g € 450,00

PEG2790.0005 5 g € 1800,00

NHO

OOH

O

O

OO

N+N

-N

8-(8-Azido-3,6-dioxaoctanoylamido)-3,6-dioxaoctanoic acid cyclohexyl-amine, Azido-AEEA-AEEA CHA FORMULA: C

12H

22N

4O

7*C

6H

13N

MOLECULAR WEIGHT: 334.33*99.17 g/moleFURTHER INFORMATION: -

PEG4170 N3-dPEG™(8)-COOH PEG4170.0100 100 mg € 350,00

PEG4170.1000 1 g € 1150,00O

O OHN37

Oalpha-Azido-omega-(propionic acid) octa(ethylene glycol) FORMULA: C

19H

37N

3O

10



PEG1405.0001 1 g € 975,00N3

OO O

O7

N

O

O

1-Azido-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-oic acid succinimidyl ester FORMULA: C

23H

40N

4O

12


PEG2015 N3-PEG(9)-COOH PEG2015.0001 1 g € 400,00

PEG2015.0005 5 g € 1350,00

N3O

NH8

OOH

O O14-azido-5-oxo-3,9,12-trioxa-6-azatetradecan-1-oic acid FORMULA: C

22H

42N

4O

12



PEG4180.1000 1 g € 1200,00O

O OHN311

Oalpha-Azido-omega-(propionic acid) dodeca(ethylene glycol) FORMULA: C

27H

53N

3O

14



PEG1395.0001 1 g € 1050,00N3

OO O

O11

N

O

O

1-Azido-3,6,9,12,15,18,21,24,27,30,33,36-dodecaoxanonatriacontan-39-oic acid succinimidyl ester FORMULA: C

31H

56N

4O

16



PEG4190.1000 1 g € 1250,00O

O OHN323

Oalpha-Azido-omega-(propionic acid) 24(ethylene glycol) FORMULA: C

51H

101N

3O

26







PEG3150 I-PEG-N3 PEG3150.0100 100 mg € 225,00

PEG3150.0500 500 mg € 625,00O

N3NH n

I

Oalpha-Iodo-omega-azido poly(ethylene glycol) (PEG-MW 3000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 Da

PEG3160 I-PEG-N3 PEG3160.0100 100 mg € 225,00

PEG3160.0500 500 mg € 625,00O

N3NH n

I


PEG3130 I-PEG-N3 PEG3130.0100 100 mg € 250,00

PEG3130.0500 500 mg € 675,00O

N3NH n

I


PEG3140 I-PEG-N3 PEG3140.0100 100 mg € 250,00

PEG3140.0500 500 mg € 675,00O

N3NH n

I


PEG2140 Biotin-PEG(3+4)-N3 PEG2140.0100 100 mg € 300,00

PEG2140.0001 1 g € 1150,00

NH

OS

NH

HN

OO

OO N

HO

OO

N33

N-(1-azido-9-oxo-3,6,14,17,20-pentaoxa-10-azatricosan-23-yl)-5-biotinami-de FORMULA: C

31H

57N

7O

10S




2 and give appropriate unwanted

impurities. The Iodo group reacts much more specifically with thiol resulting in much cleaner conjugates.

Reference:




2010; 468: 790-795.

ON3N

H n

I

O

+ I PEGR SH S PEGR




Non-specific photoreactive biotinylation reagent for non-specific labeling of organic compounds, surfaces or par-

ticles. Reacts with C-H and N-H bonds non-specifically from the photogenerated singlet nitrene with high efficiencies.

PEG2065 Biotin-TEG-ATFBA PEG2065.0025 25 mg € 300,00

PEG2065.0100 100 mg € 400,00

NH

O

S

NH

HN

OO

OO N

H

O F

F

F

F

N3

Biotin-triethylenglycol-(p-azido-tetrafluorobenzamide), 4-Azido-2,3,5,6-tetrafluoro-N-(15-oxo-19-(2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)benzamide FORMULA: C

27H

37F

4N

7O

6S


References:

f Chemistry and Kinetics of Singlet (Pentafluorophenyl)nitrene, M. S.

Platz, et al., J. Amer. Chem. Soc. 1992; 11IB4: 5054-5067.

f Synthesis and Binding of New Polyfluorinated Aryl Azides to alpha-

Chymotrypsin. New Reagents for Photoaffinity Labeling. M. S. Platz,

et al., Bioconjugate Chemistry 1993; 4: 256-261.

f Synthesis of a Tetrafluoro-Substituted Aryl Azide and Its Protio Ana-

logue as Photoaffinity Labeling Reagents for the Estrogen Receptor;

J.A. Katzenellenbogen, et al., J. Org. Chem. 1991; 56: 3125-3133.

f NHS Ester Functionalized Perfluorphenyl Azides as Novel Photoac-

tive Heterobifunctional Cross-linking Reagents. J.F.W. Keana, et al.;

Bioconjugate Chemistry 1994; 5: 151-157.

PEG4330 Biotin-dPEG™(7)-N3 PEG4330.0100 100 mg € 325,00

PEG4330.1000 1 g € 1400,00

NH

ON3

S

NH

HN

OO

7

alpha-Biotin-omega-azido hepta(ethylene glycol) FORMULA: C

26H

48N

6O

9S



PEG4340.1000 1 g € 1450,00

NH

ON3

S

NH

HN

OO

11

alpha-Biotin-omega-azido undeca(ethylene glycol) FORMULA: C

34H

64N

6O

13S



PEG4350.1000 1 g € 1600,00

NH

ON3

S

NH

HN

OO

23

alpha-Biotin-omega-azido 23(ethylene glycol) FORMULA: C

58H

112N

6O

25S



PEG4360.1000 1 g € 1800,00

23NH

OO N

HS

NH

HN

O O O

ON3

23


109H

213N

7O

50S






The broad variety of the Click reaction can be applied on surfaces using appropriate PEG-silanes, where silicate particels can be coated with.

PEG4830 Azido-PEG-Si(OMe)3 PEG4830.0500 500 mg € 500,00

PEG4830.1000 1 g € 900,00

N3O

NH

NH

nSi(OMe)3

Oalpha-Azido-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG4835.1000 1 g € 900,00

N3O

NH

NH

nSi(OMe)3



PEG4840.1000 1 g € 900,00

N3O

NH

NH

nSi(OMe)3



PEG4845.1000 1 g € 900,00

N3O

NH

NH

nSi(OMe)3


3.6 Biotin-PeG Reagents

PEG spacers eliminate the common issues of aggregation with biotinylated proteins, oligonucleotides, antibodies, and other biological materials. They provide optimal avi-din/streptavidin binding, because the PEG spacer makes the biotin very available for streptavidin in the capture/binding step.

Very water soluble, eliminates non-specific binding, non-antigenic and non-immunogenic.

Increases significantly signal to noise ration in analytical applications.

Protocol for in-situ Activation to the NHS ester:Add a methylene chloride solution of the acid to the dry reagents under dry conditions (10-20% molar excess of EDC and NHS in dry methylene chloride, dried over 3A molecular sieves). Stir for several hours or overnight, then evaporate the solvent and use. The reaction mixture can

also be treated with a small amount of silica gel to adsorb the excess EDC and the urea by-product. Filter, then evaporate the solvent and use.

NHS should be added together with EDC to prevent forma-tion of the anhydride. DCC and DIC can also be used. Typically use about 1 equivalent, and add a solution of the carbodiimide to the acid and NHS (1.1 to 1.2 eq.). PfOH (pentafluorophenol), MSNT (1-(Mesitylene-2-sulfonyl)-3-ni-tro-1,2,4-triazole), HOCt (Ethyl 1-hydroxy-1H-1,2,3-Triazole-4-carboxylate), HOPO (2-Hydroxypyridine-N-oxide) and a set of other coupling reagents/leaving groups can be used in place of NHS, if this is of any preference.

Reference:



10: 0-12-370501-0)., Ch. 18, pp. 711-742.


N3O

NH

NH

nSi(OMe)3

O




PEG2166 Biotin-PEG(4)-Lys(PEG(4)-Biotin)-PEG(4)-TFP PEG2166.0100 100 mg € 275,00

PEG2166.0001 1 g € 1200,00ONH

HNO

O

O

4

O

O

NH

O

ONH 4

NH 4

O

O

S

S

NHHN

NHHN

O

O

F

F

F

FN-alpha-N-epsilon-Bis(Biotinyl-PEG(4))-lysinyl-PEG(4)-2,3,5,6-tetrafluo-rophenyl ester FORMULA: C

65H

105F

4N

9O

21S

2

MOLECULAR WEIGHT: 1488,7 g/moleFURTHER INFORMATION: Spacers are 40 an 35 atoms and 43.4 and 41.7 A resp.

PEG4440 Fmoc-L-Lys(dPEG™(4)-Biotin)-OH PEG4440.0100 100 mg € 325,00

PEG4440.1000 1 g € 1000,00NH

OHN

S

NH

HN

O O

4O

(S)(S)OH

O

NHO

O

N-alpha-(9-Fluorenylmethyloxycarbonyl)-N-epsilon-[15-(biotinamido)-4,7,10,13-tetraoxa-pentadecanoyl]-L-lysine FORMULA: C

42H

59N

5O

11S

MOLECULAR WEIGHT: 842,01 g/moleFURTHER INFORMATION: Spacer is 19.1 atoms and 16 A

PEG4450 Fmoc-L-Lys(dPEG™(12)-Biotin)-OH PEG4450.0100 100 mg € 425,00

PEG4450.1000 1 g € 1400,00NH

OHN

S

NH

HN

O O

12O

(S)(S)OH

O

NHO

O

N-alpha-(9-Fluorenylmethyloxycarbonyl)-N-epsilon-[alpha-Biotin-ome-ga-propionyl dodeca(ethylene glycol)]-L-lysine FORMULA: C

58H

91N

5O

19S


PEG2140 Biotin-PEG(3+4)-N3 PEG2140.0100 100 mg € 300,00

PEG2140.0001 1 g € 1150,00

NH

OS

NH

HN

OO

OO N

HO

OO

N33

N-(1-azido-9-oxo-3,6,14,17,20-pentaoxa-10-azatricosan-23-yl)-5-biotinami-de FORMULA: C

31H

57N

7O

10S


Non-specific photoreactive biotinylation reagent for non-specific labeling of organic compounds, surfaces or particles. Reacts with C-H and N-H bonds non-specifically from the photogenerated singlet nitrene with high efficien-cies.

References:

f Chemistry and Kinetics of Singlet (Pentafluorophenyl)nitrene, M. S.

Platz, et al., J. Amer. Chem. Soc. 1992; 11IB4: 5054-5067.

f Synthesis and Binding of New Polyfluorinated Aryl Azides to alpha-

Chymotrypsin. New Reagents for Photoaffinity Labeling. M. S. Platz,

et al., Bioconjugate Chemistry 1993; 4: 256-261.

f Synthesis of a Tetrafluoro-Substituted Aryl Azide and Its Protio Ana-

logue as Photoaffinity Labeling Reagents for the Estrogen Receptor;

J.A. Katzenellenbogen, et al., J. Org. Chem. 1991; 56: 3125-3133.

f NHS Ester Functionalized Perfluorphenyl Azides as Novel Photoac-

tive Heterobifunctional Cross-linking Reagents. J.F.W. Keana, et al.;

Bioconjugate Chemistry 1994; 5: 151-157.

PEG2065 Biotin-TEG-ATFBA PEG2065.0025 25 mg € 300,00

PEG2065.0100 100 mg € 400,00

NH

O

S

NH

HN

OO

OO N

H

O F

F

F

F

N3

Biotin-triethylenglycol-(p-azido-tetrafluorobenzamide), 4-Azido-2,3,5,6-tetrafluoro-N-(15-oxo-19-(2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)benzamide FORMULA: C

27H

37F

4N

7O

6S


PEG1415 Biotin-dPEG™(3)-Benzophenone PEG1415.0025 25 mg € 300,00

PEG1415.0100 100 mg € 400,00

NH

OO

O NH

OO

S

HN

HN

O

ON-(3-(2-(2-(3-(Biotinamino)propoxy)ethoxy)ethoxy)propyl)-4-benzophe-none FORMULA: C

34H

46N

4O

7S



Amine reactive bis biotinylation PEGylating reagent with a PEG spacer arm with potential to polymerize avidin or

streptavidin at the label site. Very water soluble, hydro-philic and eliminates nonspecific binding.




PEG2760 Biotin-DOOA*HCl PEG2760.0250 250 mg € 200,00

PEG2760.0001 1 g € 600,00

PEG2760.0005 5 g € 2400,00

NH

OO

S

NH

HN

OO

NH2

1-Biotinyl-3,6-dioxa-8-octaneamine hydrochloride, N-{2-[2-(2-Aminoe-thoxy)ethoxy]ethoxy}biotinamide hydrochloride CAS-NO: 862373-14-6 FORMULA: C

16H

30N

4O

4S*HCl


PEG1425 Biotin-dPEG™(4)-NHNH2 PEG1425.0050 50 mg € 375,00

PEG1425.0001 1 g € 1000,00

OO

OO

NH

O

NH

O

S

NH

HN

O

NH2

15-Biotinamino-4,7,10,13-tetraoxa-pentadecanoyl hydrazide FORMULA: C

21H

39N

5O

7S


f Using Photolabile Ligands in Drug Discovery and Development; G.

Dorman, G. D. Prestwich; Trends in Biotechnology 2000; 18: 64-77.

f Benzophenone Photoprobes for Phosphoinositides, Peptides and

Drugs; G. D. Prestwich, et al.; Photochemistry and Photobiology

1997; 65(2): 222-234.

f Benzophenone Photophores in Biochemistry; G. D. Prestwich, et. al.;

Biochemistry 1993; 33(18): 5661-5673.

Biotin reagent for analytical measurements of biotin binding to streptavidin for other biotinylated species.

The reagent has been uniquely designed as a competi-tive standard reagent to assess the relative binding of biotin derivatives with avidin and streptavidin (on/off rate determinations). The 3 PEG unit chain provides an optimal binding distance and physical properties to balance the hydrophilicity of biotin.

References:

f Biotin Reagents for Antibody Pretargeting. 4. Selection of Biotin

Conjugates for in Vivo Application Based on Their Dissociation Rate

from Avidin and Streptavidin; D. Scott Wilbur, et. al.; Bioconjugate

Chemistry 2000; 11: 569-583.

f Evaluation of Biotin-Dye conjugates for Use in an HPLC Assay

To Assess Relative Binding of Biotin Derivatives with Avidin and

Streptavidin; D. Scott Wilbur, et. al.; Bioconjugate Chemistry 2000;

11: 584-598.

Carbonyl reactive biotinylation reagent, which reacts with aldehydes and ketones to give stable hydrazones in a single step and avoids reductive amination. Reacts also with activated carboxylic acids.

Prevents or eliminates aggregation when labeling large biological. Products show less non-specific binding than conventionally biotinylated compounds.

Solubility in water: >50% w/v!

Reference:



10: 0-12-370501-0). pp. 733-736: general discussion of chemistry and

properties; pg. 736: general protocol for labeling of a glycoprotein.

PEG1420 Biotin-dPEG™(3)-Cyanocobalamin PEG1420.0005 5 mg € 300,00

NH

OO

O NH

Cyanocobalamin

OO

S

HN

HN

O

Biotin-PEG(3)-Vitamin B12, N-(3-(2-(2-(3-(Biotinamino)propoxy)ethoxy)

ethoxy)propyl)-cyanocobalamin FORMULA: - MOLECULAR WEIGHT: - FURTHER INFORMATION: Spacer is 15 atoms and 18.1 A


References for the general use of benzophenone containing compounds:




Biotin-PEG-amines react with NHS and other active esters, or aldehydes/ketones in a reductive alkylation to second-ary amines. Prevent or eliminate aggregation when labeling large biologicals.

Reference and protocol:



10: 0-12-370501-0); pp. 529-530: general discussion on biotinylation;

pp. 737-738: protocol.

PEG2110 Biotin-TEG-NH2*TFA PEG2110.0100 100 mg € 250,00

PEG2110.0001 1 g € 800,00

NH

O

S

NH

HN

OO

OO NH2

N-Biotin-tetra(ethylene glycol)-diamine, N-Biotin-3,3‘-(2,2‘-oxybis(ethane-2,1-diyl)bis(oxy))dipropan-1-amine FORMULA: C

20H

38N

4O

5S*CF

3CO

2H

MOLECULAR WEIGHT: 446,60*114,02 g/moleFURTHER INFORMATION: Spacer is 15 atoms and 18.1 A

PEG4290 Biotin-dPEG™(7)-NH2 PEG4290.0100 100 mg € 375,00

PEG4290.1000 1 g € 950,00

NH

ONH2

S

NH

HN

OO

7

alpha-Biotin-omega-amino) hepta(ethylene glycol) FORMULA: C

26H

50N

4O

9S


PEG1044 Biotin-PEG(10)-NH2 PEG1044.0100 100 mg € 350,00

PEG1044.0001 1 g € 1150,00

HN

OS

NHHN

O

O

ONH2

8

alpha-Biotin-omega-amino-deca(ethylene glycol) FORMULA: C

30H

58N

4O

11S



PEG4300.1000 1 g € 1000,00

NH

ONH2

S

NH

HN

OO

11

alpha-Biotin-omega-amino) undeca(ethylene glycol) FORMULA: C

34H

66N

4O

13S


PEG4680 Biotin-dPEG™(11)-O-NH2*HCl PEG4680.0050 50 mg € 375,00

PEG4680.1000 1 g € 1375,00

11NH

O

O

S

NH

HN

O

ONH2

alpha-Biotinyl-omega-oxyamine-undeca(ethylene glycol) hydrochloride FORMULA: C

34H

66N

4O

14S



PEG4310.1000 1 g € 1150,00NH

ONH2

S

NH

HN

OO

23

alpha-Biotin-omega-amino) 23(ethylene glycol) FORMULA: C

58H

114N

4O

25S


PEG1046 Biotin-PEG-NH2 PEG1046.0500 500 mg € 375,00

PEG1046.0001 1 g € 625,00alpha-Biotin-omega-amino poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da






S

HN NH

NH

OO

NH2

O

O

n





PEG4330.1000 1 g € 1400,00

NH

ON3

S

NH

HN

OO

7

alpha-Biotin-omega-azido hepta(ethylene glycol) FORMULA: C

26H

48N

6O

9S



PEG4340.1000 1 g € 1450,00

NH

ON3

S

NH

HN

OO

11

alpha-Biotin-omega-azido undeca(ethylene glycol) FORMULA: C

34H

64N

6O

13S



PEG4350.1000 1 g € 1600,00

NH

ON3

S

NH

HN

OO

23


58H

112N

6O

25S



PEG4360.1000 1 g € 1800,00

23NH

OO N

HS

NH

HN

O O O

ON3

23


109H

213N

7O

50S


Building blocks for BIOTINIDASE RESISTANT biotinylation reagents.

For biotinylations where serum samples are being used. Biotinidase is ubiquitous in serum and will rapidly cleave biotin from the detection system. Sarcosine and 2-amino-

butyric acid are spacers resulting in derived biotinylation reagents showing a high level of resistance to biotinidase, while maintaining a high binding rate and affinity for avidin and streptavidin.


PEG2550 Biotin-Sar-OH PEG2550.1000 1 g € 375,00

NOH

S

NH

HN

OO

Me O

N-Biotinylsarcosine, N-Biotinyl-N-methyl-2-aminoacetic acid FORMULA: C

13H

21N

3O

4S


PEG2555 Biotin-2-Abu-OH PEG2555.0001 1 g € 375,00

NH

OH

S

NH

HN

OO

O

N-alpha-Biotinoyl-2-DL-aminobutyric acid FORMULA: C

14H

23N

3O

4S


References:

f Biotin Reagents for Antibody Pretargeting. 7. Investigation of Chemi-

cally Inert Biotinidase Blocking Functionalities for Synthetic Utility,”

D. Scott Wilbur, et al.; Bioconjugate Chemistry 2006; 17(6): 1514-

1522, and references therein;

f D. Scott Wilbur, et al.; Bioconjugate Chemistry 2001; 12: 616-623;

f D. Scott Wilbur, et al.; Bioconjugate Chemistry 1997; 8: 572-584.





PEG2560 Biotinyl-O2Oc-OH PEG2560.0250 250 mg € 200,00

PEG2560.0001 1 g € 600,00

PEG2560.0005 5 g € 2000,00

NH

OO

S

NH

HN

OO

OH

O

Biotinyl-AEEA, Biotinyl-Ado-OH, 8-Biotinylamido-3,6-dioxaoctanoic acid CAS-NO: 1238575-77-3 FORMULA: C

16H

27N

3O

6S


PEG2565 Biotinyl-O2Oc-O2Oc-OH PEG2565.0050 50 mg € 125,00

PEG2565.0250 250 mg € 450,00

PEG2565.0001 1 g € 1300,00

NH

OO

S

NH

HN

OOHN

O

OO

OH

O

Biotin-AEEA-AEEA-OH, Biotin-Ado-Ado-OH, 8-Biotinylamido-3,6-dioxaoc-tanoic acid dimer, 17-Biotinamido-10-oxo-3,6,12,15-tetraoxa-9-azahepta-decan-1-oic acid FORMULA: C

22H

38N

4O

9S


PEG1515 Biotin-dPEG™(4)-COOH PEG1515.0001 1 g € 650,00

OO

OO

NH

O

OH

O

S

NH

HN

O15-Biotinamino-4,7,10,13-tetraoxa-pentadecanoic acid FORMULA: C

21H

37N

3O

8S


PEG1051 Biotin-PEG(12)-COOH PEG1051.0100 100 mg € 300,00

PEG1051.0001 1 g € 1000,00NH

OS

NHHN

O

O

O11

OH

O

alpha-Biotin-omega-(propionic acid)-dodecae(ethylene glycol) FORMULA: C

37H

69N

3O

16S


PEG4260 Biotin-dPEG™(24)-COOH PEG4260.0100 100 mg € 350,00

PEG4260.1000 1 g € 1400,00

23NH

OO OH

S

NH

HN

O O O

alpha-Biotin-omega-(propionic acid) 24(ethylene glycol) FORMULA: C

61H

117N

3O

28S


PEG4270 Biotin-dPEG™(48)-COOH PEG4270.0100 100 mg € 425,00

PEG4270.1000 1 g € 1550,00

23NH

OO N

HS

NH

HN

O O O

O OH

24 O

alpha-Biotin-omega-(propionic acid) 48(ethylene glycol) FORMULA: C

112H

218N

4O

53S


PEG1053 Biotin-PEG-COOH PEG1053.0500 500 mg € 420,00

PEG1053.0001 1 g € 720,00S

HN NH

NH

OO

O

O

n

OH

Oalpha-Biotin-omega-carboxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG1054.0001 1 g € 720,00S

HN NH

NH

OO

O

O

n

OH



PEG1052.0001 1 g € 775,00S

HN NH

NH

OO

O

O

n

OH



S

HN NH

NH

OO

O

O

n

OH

O




PEG1525 Fmoc-NH-(dPEG™(4)-Biotin)-COOH PEG1525.0100 100 mg € 375,00

PEG1525.0001 1 g € 1150,00NH

OO

OO N

OO

OH

S

HN

HN

O O

NHO

O

3-[15-(Biotinamido)-4,7,10,13-tetraoxa-pentadecanamido]-3-[(9-fluoren-methyl)ethylcarbamate]-propanoic acid FORMULA: C

41H

57N

5O

11S

MOLECULAR WEIGHT: 827,98 g/moleFURTHER INFORMATION: Spacer is 19.1 atoms and 16 A

PEG2070 Biotin-TEG-OPfp PEG2070.0050 50 mg € 250,00

PEG2070.0001 1 g € 700,00

NH

OO

S

NH

HN

OO

OO

O

O

F

F

F

F

F

Biotin-tetra(ethylene glycol)-pentafluorphenyl ester, Pentyfluorophenyl 17-oxo-21-(2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10,13-tetrao-xa-16-azahenicosan-1-oate FORMULA: C

27H

36F

5N

3O

8S


PEG1870 Biotin-dPEG™(4)-NHS PEG1870.0050 50 mg € 250,00

PEG1870.0001 1 g € 800,00

NOO

ONH

O

S

NH

HN

O

3

OO

O

15-Biotinamino-4,7,10,13-tetraoxa-pentadecanoic acid succinimidyl ester FORMULA: C

25H

40N

4O

10S



Protocol:The pegylation reagent can be pre-dissolved in an organic solvent or can be directly dissolved in pure water, but must be used immediately. The reaction is best run be-tween pH 7.2 and 8 using a non-amine buffer, e.g., PBS pH 7.2. Typical incubation times will be about 2 hours on ice and 30 minutes at RT. For large molecules the unreacted biotinylation reagent can be removed with gel filtration or dialysis.

References:

f Biotin Reagents for Antibody Pretargeting. 7. Investigation of Chemi-

cally Inert Biotinidase Blocking Functionalities for Synthetic Utility,”

D. Scott Wilbur, et al.; Bioconjugate Chemistry 2006; 17(6): 1514-1522,

and references therein;

f D. Scott Wilbur, et al.; Bioconjugate Chemistry 2001; 12: 616-623;

f D. Scott Wilbur, et al.; Bioconjugate Chemistry 1997; 8: 572-584.

BIOTINIDASE RESISTANT amine reactive biotinylation PEGylation reagent especially for in vivo experiments or clinical analysis. For biotinylations where serum samples are being used. Biotinidase is ubiquitous in serum and will rapidly cleave biotin from the detection system.

Very water soluble, hydrophilic and eliminates non-specif-ic binding. Non-antigenic, non-immunogenic.

The PEGylation arm of this spacer gives optimal biotin binding with streptavidin conjugates; chain length from amide to terminal carbonyl is 19.2 Angstroms. Designed to be the same length as the LC-LC spacer, which is ideal for the streptavidin binding pocket.

Will significantly increase signal to noise ration in analyti-cal applications.

PEG1845 Biotin-dPEG™(4)-NHS-(Biotinidase resistant) PEG1845.0100 100 mg € 275,00

PEG1845.0001 1 g € 1250,00

NH

HN

OO O

N

O

OS

HN

HN

O

3O

O

O

18-Biotinamino-17-oxo-4,7,10,13-tetraoxa-16-azaicosan-1-oic acid succini-midyl ester FORMULA: C

29H

47N

5O

11S






Amine reactive biotinylation reagent with cleavable PEGylation spacer for more effective binding, availability and solubility. The disulfide moiety provides cleaving pos-sibilities for sophisticated experiments.

Very water soluble, hydrophilic and eliminates nonspe-cific binding. Non-antigenic and non-immunogenic.

PEG1910 Biotin-dPEG™(4)-S-S-NHS PEG1910.0050 50 mg € 300,00

PEG1910.0500 500 mg € 900,00

3NH

OO N

HS

SS

NH

HN

OO O

ON

OO

O

1-Biotinamino-15-oxo-3,6,9,12-tetraoxa-19,20-dithia-16-azatricosan-23-oic acid succinimidyl ester FORMULA: C

30H

49N

5O

11S

3


Eliminates aggregation and precipitation when labeling antibodies and other biological materials.

The chain length from amide to terminal carbonyl is 28.7 Angstroms or 24 atoms, which is ideal for the streptavidin binding pocket.

Protocol:Can be used directly in water, but should be dissolved in organic solvent for optimal and easiest application.

Reference:



10: 0-12-370501-0), pp. 726-729.

Biotin-PEG-S-S-NHS can be used to label a primary an-tibody molecule that has specificity for a certain protein. Incubation of the biotinylated antibody with a sample, such as a cell lysate, allows the antibody to bind to its target. Capture of the antibody-antigen complex on an immobilized streptavidin reagent effectively isolates the target protein from the other proteins in the sample. The

disulfide linkage in the spacer arm of the biotin tag per-mits elution of the immune complex from the streptavidin support under mild conditions by using DTT. Otherwise strong denaturating conditions typically required to break the streptavidin-biotin interaction have to be applied.

SSNH2 + PEGO

N

OO

O

HN

O

S

NHHN

O

SS

PEGNH

OHN

O

S

NHHN

O

SSNH2 + PEGO

N

OO

O

HN

O

S

NHHN

O

SS

PEGNH

OHN

O

S

NHHN

O

SS

PEGNH

OHN

O

SNH

NHO

HSSH PEGNH

OHN

O

SNH

NHO

streptavidin-biotin complex

antibody- antigen complex

DTT





PEG1860.0001 1 g € 1300,00

11NH

OO O

N

S

NH

HN

O O OO

O

alpha-Biotin-omega-carboxy succinimidyl ester dodeca(ethylene glycol) FORMULA: C

41H

72N

4O

18S



PEG4250.1000 1 g € 1450,00

23NH

OO O

N

S

NH

HN

O O OO

O

alpha-Biotin-omega-(succinimidyl propionate) 24(ethylene glycol) FORMULA: C

65H

120N

4O

30S


PEG1056 Biotin-PEG-NHS PEG1056.0100 100 mg € 140,00

PEG1056.0500 500 mg € 475,00

PEG1056.0001 1 g € 830,00

S

HN NH

NH

OO

O

O

n

O

O

N

O

O

alpha-Biotin-omega-carboxy succinimidyl ester poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1057.0001 1 g € 830,00S

HN NH

NH

OO

O

O

n

O

O

N

O

O



PEG1055.0500 500 mg € 500,00

PEG1055.0001 1 g € 900,00

S

HN NH

NH

OO

O

O

n

O

O

N

O

O


PEG1206 Biotin-PEG-OH PEG1206.0500 500 mg € 650,00

PEG1206.0001 1 g € 1100,00S

HN NH

NH

OO

OH

O

O

n

alpha-Biotin-omega-hydroxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -

PEG1207 Biotin-PEG-OH PEG1207.0500 500 mg € 650,00

PEG1207.0001 1 g € 1100,00S

HN NH

NH

OO

OH

O

O

n

alpha-Biotin-omega-hydroxy poly(ethylene glycol) (PEG-MW 5.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 5000 DaFURTHER INFORMATION: -

PEG4705 Biotin-PEG(11)-SH PEG4705.0100 100 mg € 450,00

PEG4705.1000 1 g € 1300,00S

HN NH

NH

OO

SH

O

O

10alpha-Biotin-omega-mercapto undeca(ethylene glycol) FORMULA: C

34H

65N

3O

13S

2



S

HN NH

NH

OO

O

O

n

O

O

N

O

O

S

HN NH

NH

OO

OH

O

O

n




PEG1213 Biotin-PEG-SH PEG1213.0100 100 mg € 350,00

PEG1213.0500 500 mg € 1050,00

PEG1213.0001 1 g € 1950,00

S

HN NH

NH

OO

HN

O

O

n O

SHalpha-Biotin-omega-mercapto poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1214.0500 500 mg € 1050,00

PEG1214.0001 1 g € 1950,00

S

HN NH

NH

OO

HN

O

O

n O



PEG1212.0500 500 mg € 1100,00

PEG1212.0001 1 g € 2000,00

S

HN NH

NH

OO

HN

O

O

n O



PEG1226.0500 500 mg € 1100,00

PEG1226.1000 1 g € 2000,00

S

HN NH

NH

OO

HN

O

O

n O


PEG4770 Biotin-PEG-OPSS PEG4770.0500 500 mg € 800,00

PEG4770.1000 1 g € 1400,00S

HN NH

NH

OO

HN

O

O

n O

SS N

alpha-Biotin-omega-pyridyl-2-disulfid poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG4775.1000 1 g € 1400,00S

HN NH

NH

OO

HN

O

O

n O

SS N



PEG4780.1000 1 g € 1400,00S

HN NH

NH

OO

HN

O

O

n O

SS N



PEG4785.1000 1 g € 1400,00S

HN NH

NH

OO

HN

O

O

n O

SS N



S

HN NH

NH

OO

HN

O

O

n O

SH

S

HN NH

NH

OO

HN

O

O

n O

SS N




PEG1605 Biotin-dPEG™(3)-mal PEG1605.0050 50 mg € 325,00

NH

OO

O NH

O

N

O

S

NHHN

OO

O

N-(3-(2-(2-(3-(Biotinamino)propoxy)ethoxy)ethoxy)propyl)-3-maleinimi-dylpropanamide FORMULA: C

27H

43N

5O

8S



PEG1595.0100 100 mg € 575,00NH

ONH

S

NH

HN

OO

11

O

N

O

O

alpha-Biotin-omega-maleinimido undeca(ethylene glycol) FORMULA: C

41H

71N

5O

16S



PEG4320.0100 100 mg € 600,00NH

ONH

S

NH

HN

OO

23

O

N

O

O

alpha-Biotin-omega-maleinimido) 23(ethylene glycol) FORMULA: C

65H

119N

5O

28S


PEG1049 Biotin-PEG-mal PEG1049.0500 500 mg € 500,00

PEG1049.0001 1 g € 850,00S

HN NH

NH

ONH

O

O

n

N

OO

O

alpha-Biotin-omega-maleinimido poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1050.0001 1 g € 850,00S

HN NH

NH

ONH

O

O

n

N

OO

O



PEG1048.0001 1 g € 900,00S

HN NH

NH

ONH

O

O

n

N

OO

O


Conventional thiol reactive biotinylation reagents are very hydrophobic, which limits practical and commercial use due to low solubility, aggregation and precipitation of biotinylated species.

PEGylation spacer makes the reagent water soluble, eliminates non-specific binding in the application and increases signal to noise ratio in analytical measurements. Non-antigenic and non-immunogenic.

Biotinylates sulfhydryl containing peptides and proteins or terminal sulfhydryl modified DNA at acidic to neutral pH, due to the high reactivity of the maleimide with thiols/sulfhydryls. In solution there are no aggregation or pre-cipitation problems when labeling antibodies and other biological material.

Longer spacer may allow biotin accessibility of the biotin by the streptavidin/avidin conjugate binding system where the reactive thiols are buried in the labeled system, away from the surface.

Protocols & References:



10: 0-12-370501-0). pp. 732-733.

f D. Scott Wilbur, et. al., “Biotin Reagents for Antibody Pretargeting. 3.

Sythesis Radioiodination, and Evaluation of Biotinylated Starburst

Dendrimers”; Bioconjugate Chemistry 1998; 11: 813-825.

f D. Scott Wilbur, et. al., “Biotin Reagents for Antibody Pretargeting.

2. Synthesis and in Vitro Evaluation of Biotin Dimers and Trimers

for Cross-Linking of Streptavidin”; Bioconjugate Chemistry 1997; 11: 819-832.


S

HN NH

NH

ONH

O

O

n

N

OO

O




PEG2080 Biotin-TEG-Biotin PEG2080.0050 50 mg € 300,00

PEG2080.0001 1 g € 775,00

NH

OS

NH

HN

OO

OO N

H

O

SNH

HNO

N,N‘-Bisbiotin-tetra(ethylene glycol)-diamine, 3,3‘-(2,2‘-Oxybis(ethane-2,1-diyl)bis(oxy))dipropan-1-amido-biotin FORMULA: C

30H

52N

6O

7S

2


PEG4850 Biotin-PEG-Si(OMe)3 PEG4850.0500 500 mg € 500,00

PEG4850.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3

OO

S

NH

HN

Oalpha-Biotinyl-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG4855.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3

OO

S

NH

HN



PEG4860.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3

OO

S

NH

HN



PEG4865.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3

OO

S

NH

HN

O

alpha-Biotinyl-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 20.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 20000 DaFURTHER INFORMATION: -

3.7 PeG-thiols

3.7.1 Lipoamide-PeGsNanotechnology and nanobiotechnology using gold or silver particles, quantum dots or even magnetic particles are broadly diverse, rapidly expanding areas of study in medical diagnostics and therapeutics, sensoric and chemistry. Metal particles, however, are not water soluble without further modification. Thiols readily form dative bonds to gold and silver surfaces creating self-assembled monolayers (SAMs), which modify surfaces for coupling proteins and other molecules. Monothiols, however, can be readily removed by reducing agents such as DTT (Cleland’s Reagent). The disulfide lipoic acid (also known as thioctic acid) binds far stronger to metal surfaces and is much more resistant towards removal from the metal surface by DTT and similar reagents than monothiols.

PEG linkers impart hydrophilicity, non-antigenicity and non-immunogenicity to nanoparticles. With the methoxy-capped PEG linker a water shell can be created around the nanoparticle. Lipoamido-PEG-acids and lipoamido-PEG-alcohols can be used as intermediates for derivatizing the PEG linker after attaching to the surface. A co-coating with methoxy-PEG-lipoamides will specifically reduce the density of functional groups on the surface. This is essen-tial, if interaction with large molecules like proteins and antibodies is expected.

Stench is often operative for thiols! Lipoic acid derivatives, however, have NO ODOR.


NH

ONH

NH

nSi(OMe)3

OO

S

NH

HN

O




SS

PEG

NH

O

O

S S

PEG

NH

O

O

S S

PEG

NH

O

O

SS

PEG

NHO

O

Protocol:A variety of protocols exist in the literature and on various websites for reducing lipoic acid (LA) to dihydrolipoic acid (DHLA). Both Tris(2-carboxyethyl)phosphine (TCEP) and sodium borohydride (NaBH4) have been used success-fully for reduction of LA to DHLA. For specific procedures, please consult literature. In general, TCEP reduction is carried out in water or aqueous buffer (excluding phos-phate buffer, in which TCEP is unstable), in three times or greater molar excess to the lipoic acid derivative, using an incubation temperature of 25°C to 50°C, for about 1-2 hours. Each reduction procedure must be optimized for the particular lipoic acid derivative being reduced to the corresponding DHLA derivative.

References:

f Greg T. Hermanson. Bioconjugate Techniques, 2nd edition. Elsevier,

Inc., Burlington, MA 01803, April 2008 (ISBN-13: 978-0-12-370501-3;

ISBN-10: 0-12-370501-0), pp. 188-190, 485-497, 924-935.

f Prime and Whitesides, Self-assembled organic monolayers: model

systems for studying adsorption of proteins at surfaces, Science

1991; 252: 1164-1167.

f Sapsford, et al. Biosensing with luminescent semiconductor quan-

tum dots. Sensors 2006; 6: 925-953.

f Dougan, et al. Enhanced oligonucleotide–nanoparticle conjugate

stability using thioctic acid modified Oligonucleotides; Nucleic

Acids Research 2007; 35(11): 3668-3675.

f Sharma, et al., Toward reliable gold nanoparticle patterning on

self-assembled DNA nanoscaffold; J. Am.Chem. Soc. 2008; 130: 7820–7821.

f Satoh, et al., Simultaneous determination of α-lipoic acid and its

reduced form by high-performance liquid chromatography with

fluorescence detection; Journal of Chromatography B 2007; 854: 109–115.

f Toyo’oka. Recent advances in separation and detection methods for

thiol compounds in biological samples; Journal of Chromatography

B 2009; 877: 3318-3330.

f Tai Hwan Ha, et al., Oriented Immobilization of Antibodies with

GSTFused Multiple Fc-Specific B-Domains on a Gold Surface; Anal.

Chem. 2007; 79: 546-556.

f Kimihiro Susumu, et al., Design of Biotin-Functionalized Lumines-

cent Quantum Dots; J. of Biomedicine and Biotechnology 2007;

Article ID 90651.

f Bing C. Mei, et al., Polyethylene glycol-based bidentate ligands to

enhance quantum dot and gold nanoparticle stability in biological

data; Nature Protocols 2009; 4(3): 412-423.

f Guodong Zhang, et al., Influence of anchoring ligands and particle

size on the colloidal stability and in vivo biodistribution of polyeth-

ylene glycol-coated gold nanoparticles in tumor-zenografted mice.

Biomaterials 2009; 30: 1928-1936.

f Bing C. Mei, et al., Modular poly (ethylene glycol) ligands for bio-

compatible semiconductor and gold nanocrystals with extended pH

and ionic stability; J. of Materials Chemistry 2008; 18: 4949-4958.




PEG3500 Lipoamide-dPEG™(4)-COOH PEG3500.0100 100 mg € 325,00

PEG3500.1000 1 g € 850,00O

O3

OH

O

NH

O

S S

alpha-Lipoamide-omega-(propionic acid) tetra(ethylene glycol) FORMULA: C

19H

35NO

7S

2



PEG3510.1000 1 g € 1200,00O

O7

OH

O

NH

O

S S

alpha-Lipomide-omega-(propionic acid) octa(ethylene glycol) FORMULA: C

27H

51NO

11S

2



PEG3520.1000 1 g € 1300,00O

O11

OH

O

NH

O

S S

alpha-Lipoamide-omega-(propionic acid) dodeca(ethylene glycol) FORMULA: C

35H

67NO

15S

2



PEG3530.1000 1 g € 1350,00O

O15

OH

O

NH

O

S S

alpha-Lipoamide-omega-(propionic acid) hexadeca(ethylene glycol) FORMULA: C

43H

83NO

19S

2



PEG3540.1000 1 g € 1450,00O

O23

OH

O

NH

O

S S

alpha-Lipoamide-omega-(propionic acid) 24(ethylene glycol) FORMULA: C

59H

115NO

27S

2


PEG3570 Lipoamide-dPEG™(3)-biotin PEG3570.0100 100 mg € 375,00

PEG3570.1000 1 g € 1000,00

OO

2NH

O

S S

HN

O

S

NHHN

Oalpha-Lipoamide-omega-biotinyl tri(ethylene glycol) FORMULA: C

28H

50N

4O

6S

3


PEG3580 Lipoamide-dPEG™(11)-biotin PEG3580.0100 100 mg € 450,00

PEG3580.1000 1 g € 1300,00O

NH11

NH

O

S S

O

S

NH

HNO

alpha-Lipoamide-omega-biotinyl undeca(ethylene glycol) FORMULA: C

42H

78N

4O

14S

3






PEG3590 Lipoamide-dPEG™(4)-OMe PEG3590.0100 100 mg € 275,00

PEG3590.1000 1 g € 750,00O

OMe3

NH

O

S S

alpha-Lipoamide-omega-methoxy tetra(ethylene glycol) FORMULA: C

17H

33NO

5S

2



PEG3600.1000 1 g € 1000,00O

OMe7

NH

O

S S

alpha-Lipoamide-omega-methoxy octa(ethylene glycol) FORMULA: C

25H

49NO

9S

2

MOLECULAR WEIGHT: 571,79 g/moleFURTHER INFORMATION: Spacer length 34.5 atoms or 38.8 A


PEG3610.1000 1 g € 1200,00O

OMe11

NH

O

S S

alpha-Lipoamide-omega-methoxy dodeca(ethylene glycol) FORMULA: C

33H

65NO

13S

2

MOLECULAR WEIGHT: 748 g/moleFURTHER INFORMATION: Spacer length 46 atoms or 53.3 A


PEG3620.1000 1 g € 1350,00O

OMe23

NH

O

S S

alpha-Lipoamide-omega-methoxy 20(ethylene glycol) FORMULA: C

57H

113NO

25S

2


PEG3550 Lipoamide-dPEG™(3)-mal PEG3550.0100 100 mg € 350,00

PEG3550.1000 1 g € 950,00

OO

2NH

O

S S

HN N

O

O

O

alpha-Lipoamide-omega-maleinimido tri(ethylene glycol) FORMULA: C

25H

41N

3O

7S

2


PEG3560 Lipoamide-dPEG™(11)-mal PEG3560.0100 100 mg € 425,00

PEG3560.1000 1 g € 1150,00O

NH11

NNH

O

S S

O O

O

alpha-Lipoamide-omega-maleinimido undeca(ethylene glycol) FORMULA: C

39H

69N

3O

15S

2


Maleimide provides functionality for antibody immobilization, as well as peptides, and oligonucleotides.






Cleland‘s reagent, also known as DL-Dithiothreitol or DTT is deprotecting thiolated DNA. The terminal sulfurs of thiolated DNA have a tendency to oxidize and form dimers in solution, especially in the presence of oxygen. Dimerization significantly lowers the efficiency of subse-quent coupling reactions such as DNA immobilization on gold surfaces in biosensors. Normally DTT is mixed with a DNA solution and allowed to react, and then is removed by filtration (solid catalyst) or by chromatography (liquid form). The DTT removal procedure is also commonly called „desalting.“ DTT is frequently used to reduce the di-sulfide bonds of proteins and, in order to prevent intramo-

lecular (cyclization) and intermolecular (oligomerisation, polymerisation) disulfide bonds from cysteine residues of proteins. However, DTT cannot reduce solvent-inaccessible disulfide bonds. Therefore reduction of disulfide bonds is sometimes carried out under denaturing conditions (e.g., at high temperatures, or in the presence of a strong dena-turating agents such as 6 M guanidinium hydrochloride, 8 M urea, or 1% sodium dodecylsulfate). Contrariwise, the solvent exposure of different disulfide bonds can be as-sayed by their rate of reduction in the presence of DTT.

Our production process does not involve carcinogenic intermediates. It is therefore a safe process, taking care of the integrity of environment and of the health of all personal involved in production and handling.

RL-1020 DTT (racemic) RL-1020.0025 25 g € 200,00

RL-1020.0100 100 g € 275,00

HSSH

OH

OH

HSSH

OH

OH

Cleland‘s Reagent, DL-Dithiothreitol, (2S,3S;2R,3R)-threo-1,4-Dimercap-to-2,3-butandiol CAS-NO: 3483-12-3 FORMULA: C

4H

10O

2S

2


Literature:

f Dithiothreitol, A New Protective Reagent for SH Groups; Cleland,

W.W.; Biochemistry; April 1964; 3: 480–2. doi:10.1021/bi00892a002.

f Cleavage of disulfide bonds in proteins; Ruegg, UT; Rudinger, J.;

Methods Enzymol 1977; 47: 111.

f From Production of Peptides in Milligram Amounts for Research to

Multi-Tons Quantities for Drugs of the Future; Thomas Bruckdor-

fer, Oleg Marder and Fernando Albericio; Current Pharmaceutical

Biotechnology 2004; 5: 29-43.

Bulk Quantities are under continuous production.

Ton lot quantities are available within short delivery time.





Protocol for in-situ Activation of PEG-Acids to the NHS ester:Add a methylene chloride solution of the acid to the dry reagents under dry conditions (10-20% molar excess of EDC and NHS in dry methylene chloride, dried over 3A molecular sieves). Stir for several hours or overnight, then evaporate the solvent and use. The reaction mixture can also be treated with a small amount of silica gel to adsorb the excess EDC and the urea by-product. Filter, then evaporate the solvent and use.

NHS should be added together with EDC to prevent forma-tion of the anhydride. DCC and DIC can also be used. Typically use about 1 equivalent, and add a solution of

the carbodiimide to the acid and NHS (1.1 to 1.2 eq.). PfOH (pentafluorophenol), MSNT (1-(Mesitylene-2-sulfonyl)-3-ni-tro-1,2,4-triazole), HOCt (Ethyl 1-hydroxy-1H-1,2,3-Triazole-4-carboxylate), HOPO (2-Hydroxypyridine-N-oxide) and a set of other coupling reagents/leaving groups can be used in place of NHS, if this is of any preference.

Reference:



10: 0-12-370501-0)., Ch. 18, pp. 711-742.

3.7.2 Mercapto-PeG-Acids

S-Acetyl-PEG-acids and active esters provide a method for converting amino groups to a thiol, while incorporat-ing PEG units. Conjugation with thiol reactive agents e.g., maleimides, vinyl sulfones or α-halo keto functionalized reaction partners increases the conjugation possibilities of

the former amino group by the whole set of thiol reactive reagents.

Highly hydrophilic, non-antigenic, non-immunogenic and non-toxic.

Reference:

f Greg T. Hermanson, Bioconjugate Techniques, 2nd Ed, Elsevier Inc., Burlington, MA 01803, April, 2008 (ISBN-13: 978-0-12-370501-3; ISBN-10:

0-12-370501-0); pg. 71: general description and use; pg. 795: modification of antibodies; pg. 984 modification of amines on nucleotides and DNA

probes; pg. 90,909, and 919: modification of enzymes, reactions with avidin and streptavidin.

O

O

N

O

O

SMe

ONH2 +

PEG

NH

O

SMe

O

PEG

NH

O

SHPEG+ HO-NH2

- HO-NH-Ac

NH

O

SPEG+ MAL-antibody

N

O

O




PEG1940 Ac-S-dPEG™(4)-COOH PEG1940.0100 100 mg € 350,00

PEG1940.0001 1 g € 1100,00OO

OO

S

O

OH

O

15-Acetylthio-4,7,10,13-tetraoxa-pentadecanoic acid FORMULA: C

13H

24O

7S


PEG1945 Ac-S-dPEG™(4)-NHS PEG1945.0100 100 mg € 350,00

PEG1945.0001 1 g € 1150,00OO

OO

S

O

O

O

N

O

O

15-Acetylthio-4,7,10,13-tetraoxa-pentadecanoic acid succinimidyl ester FORMULA: C

17H

24NO

9S



PEG1950.0001 1 g € 1100,00SO 8 OH

O

O

1-Acetylthio-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-oic acid FORMULA: C

21H

40O

11S



PEG1955.0001 1 g € 1150,00

SO

8O

O

O

N

O

O

1-Acetylthio-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-oic acid succini-midyl ester FORMULA: C

25H

43NO

13S



PEG3660.1000 1 g € 1300,00OS

O

OH

12

Oalpha-Acethylthio-omega-(propionic acid) dodeca(ethylene glycol) FORMULA: C

29H

56O

15S



PEG3630.1000 1 g € 1350,00O

S

O

ON

O

O

12

Oalpha-Acethylthio-omega-(succinimidyl propionate) dodeca(ethylene glycol) FORMULA: C

33H

59NO

17S



PEG3670.1000 1 g € 1400,00OS

O

OH

16

Oalpha-Acethylthio-omega-(propionic acid) hexadeca(ethylene glycol) FORMULA: C

37H

72O

19S



PEG3640.1000 1 g € 1400,00OS

O

ON

O

O

16

Oalpha-Acethylthio-omega-(succinimidyl propionate) hexadeca(ethylene glycol) FORMULA: C

41H

75NO

21S



PEG3680.1000 1 g € 1500,00OS

O

OH

20

Oalpha-Acethylthio-omega-(propionic acid) 20(ethylene glycol) FORMULA: C

45H

88O

23S



PEG3650.1000 1 g € 1450,00O

S

O

ON

O

O

20

Oalpha-Acethylthio-omega-(succinimidyl propionate) 20(ethylene glycol) FORMULA: C

49H

91NO

25S






PEG1970 HS-dPEG™(4)-COOH PEG1970.0100 100 mg € 325,00

PEG1970.0001 1 g € 800,00

HSO 4 OH

O15-Mercapto-4,7,10,13-tertaoxa-pentadecanoic acid FORMULA: C

11H

22O

6S


PEG1980 Trt-S-dPEG™(4)-COOH PEG1980.0100 100 mg € 275,00

PEG1980.0001 1 g € 650,00O

OO

OS

O

OH

15-Tritylthio-4,7,10,13-tertaoxa-pentadecanoic acid FORMULA: C

30H

36O

6S


PEG1740 Mmt-S-dPEG™(4)-COOH PEG1740.0100 100 mg € 275,00

PEG1740.0001 1 g € 600,00S

O 4 OH

O

MeO

15-(4-Methoxytrityl)thio-4,7,10,13-tertaoxa-pentadecanoic acid FORMULA: C

31H

38O

7S


PEG1120 HS-PEG(8)-COOH PEG1120.0001 1 g € 400,00

PEG1120.0005 5 g € 1450,00

HSO 8 OH

Oalpha-Thio-omega-(propionic acid) octa(ethylene glycol) FORMULA: C

19H

38O

10S



PEG1735.0001 1 g € 950,00S

O 8 OH

O

MeO

alpha-(4-Methoxytrityl)thio-octa(ethylene glycol)-omega-propionic acid FORMULA: C

39H

54O

11S



PEG3440.1000 1 g € 1300,00

HSO 12 OH

Oalpha-Thio-omega-(propionic acid) dodeca(ethylene glycol) FORMULA: C

27H

54O

14S


Bifunctional thiol-PEG-acids attach to Au and Ag surfaces and equip them with hydrophilic properties and carboxyl functionality, which can be used for further derivatization.

PEG-thiols are reactive with metal surfaces, other thiols, disulfides, maleimides, vinyl sulfones, and haloacet-amides, incorporate water solubility, reduce or eliminate aggregation, and are inherently non-immunogenic and non-toxic.

Useful PEGylating reagents for incorporating the sulfhydryl moiety into a peptide, potentially an alternative to cyste-ine in peptide sequences.

Very soluble in methylene chloride and ethyl acetate.

Product handling and stability:Keep product under an inert atmosphere (dry nitrogen or argon recommended) to prevent oxidation to the disulfide!

Deprotection conditions for trityl derivatives:Trt (Trityl) is removed using 25-50% TFA with 5% TIS (triisopropyl silane).

Mmt (4-Methoxy-trityl) can be removed with <5% TFA in the presence of TIS (triisopropyl silane).

Reference:



10: 0-12-370501-0).






PEG4600.1000 1 g € 1100,00S

O12

OH

O

MeO

alpha-(4-Methoxytrityl)thio-dodeca(ethylene glycol)-omega-propionic acid FORMULA: C

47H

70O

15S



PEG3450.1000 1 g € 1300,00HS

O 16 OH

Oalpha-Thio-omega-(propionic acid) hexadeca(ethylene glycol) FORMULA: C

35H

70O

18S



PEG4610.1000 1 g € 1250,00S

O16

OH

O

MeO

alpha-(4-Methoxytrityl)thio-hexadeca(ethylene glycol)-omega-propionic acid FORMULA: C

55H

86O

19S



PEG3460.1000 1 g € 1450,00HS

O 20 OH

Oalpha-Thio-omega-(propionic acid) 20(ethylene glycol) FORMULA: C

43H

86O

22S



PEG4620.1000 1 g € 1350,00S

O20

OH

O

MeO

alpha-(4-Methoxytrityl)thio-20(ethylene glycol)-omega-propionic acid FORMULA: C

63H

102O

23S


PEG1119 HOOC-PEG(8)-SS-PEG(8)-COOH PEG1119.0001 1 g € 475,00

PEG1119.0005 5 g € 1500,00S

O 8 OH

O

2

Propionic acid octa(ethylene glycol)-disulfid CAS-NO: 873013-93-5 FORMULA: C

38H

74O

20S

2


PEG1188 NHS-PEG(8)-SS-PEG(8)-NHS PEG1188.0001 1 g € 550,00

PEG1188.0005 5 g € 1775,00

SO 8 O

O

2

N

O

O

N-Hydroxy-succinimidy-propionate octa(ethylene glycol)-disulfid CAS-NO: 947601-98-1 FORMULA: C

46H

80N

2O

24S

2


PEG2000 HS-FA-PEG(12)-COOH PEG2000.0100 100 mg € 450,00

HN

O 12 OH

O

HS

O

alpha-(11-Mercapto-undecanoylamido)-omega-carboxy dodeca(ethylene glycol) FORMULA: C

38H

75NO

15S


PEG2005 HS-FA-PEG(28)-COOH PEG2005.0100 Please inquire!

HN

O 28 OH

O

HS

O

alpha-(11-Mercapto-undecanoylamido)-omega-carboxy 28(ethylene glycol) FORMULA: C

70H

139NO

31S






PEG1099 HS-PEG-COOH PEG1099.0500 500 mg € 325,00

PEG1099.0001 1 g € 550,00

NH

O O OH

O

O

HSn

alpha-Thio-omega-carboxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1100.0001 1 g € 550,00

NH

O O OH

O

O

HSn



PEG1098.0001 1 g € 600,00

NH

O O OH

O

O

HSn


PEG1200 Trt-S-PEG-NHS PEG1200.0500 500 mg € 500,00

PEG1200.0001 1 g € 900,00NH

O O O

O

O

S N

O

On

alpha-Tritylthio-omega-carboxy succinimidyl ester poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1201.0001 1 g € 900,00NH

O O O

O

O

S N

O

On



PEG1199.0001 1 g € 950,00NH

O O O

O

O

S N

O

On



NH

O O OH

O

O

HSn

NH

O O O

O

O

S N

O

On





The general application of OPSS protected mercapto-PEG crosslinkers is the controlled and selective conjugation of an amine containing target, which reacts first with the NHS ester and then subsequently with a sulfhydryl containing complementary target molecule to form another disul-fide. Many biological molecules contain both the amine function and the complementary compounds. Peptides, oligonucleotides or other biologicals, for example, can be terminated with thiols or have thiols designed into them, and vice versa. The contrast with the maleimide containing crosslinkers is that the OPSS derivatives form a disulfide, stable under non-reducing conditions. Normally thiols can be cleaved with a reducing agent, or exchanged with another thiol.

The OPSS group presents the potential of using the pyridine-2-thione, released in the reaction with another thiol, to measure the level of the PEG-OPSS incorporation in the labeling step or to monitor the subsequent reaction with another thiol by measuring its absorption at 343 nm.

The cleavable OPSS PEGylating reagents produce a disul-fide bond with thiols, which can later be cleaved with a variety of reducing agents, like DTT or TCEP, or react with another thiol.

References:



10: 0-12-370501-0), pp. 276-335, 286-288, 1192-1193.

f M. Zhao, et al.; Bioconjugate Chemistry 2002; 13: 840-844.

f D.H.Na, et al.; Bioconjugate Chemistry 1999; 10: 306-310.

f S. Kamruzzahan, et al.; Bioconjugate Chemistry 2006; 17: 1473.

f K. Patri, et al.; Bioconjugate Chemistry 2004; 15: 1174-1181.

f H. J. Gruber, et al.; Bioconjugate Chemistry 2000; 11: 161-166.

f N. J. Davimandan, et al.; Bioconjugate Chemistry 2006; 17: 1376-

1384.

f M. Heggli, et al.; Bioconjugate Chemistry 2003; 14: 967-973.

f S. B. Rajur et al.; Bioconjugate Chemistry 1997; 8: 935-940.

O

SS N

O

NH2 + PEG

NH

O

PEG

1. reduction via DTT, TCEP, TE2. + MAL-Reaction Partner

SS N

O

ON

O

O

+ HS-Reaction Partner

O

SS

NH

O

PEG

O

SNH

O

PEG

R

N

O

O

O

HN R

= enzyme, protein, 5'-amino-oligonucleotide, antibody




PEG2225 OPSS-PEG(4)-COOH PEG2225.0100 100 mg € 375,00

PEG2225.0001 1 g € 1000,00O

O OHNH

SS

O

3

O

N

N-[3-(o-Pyridyldisulfido)propanoyl]-15-amino-4,7,10,13-tetraoxa-pentade-canoic acid FORMULA: C

19H

30N

2O

7S

2


PEG2230 OPSS-PEG(4)-NHS PEG2230.0100 100 mg € 375,00

PEG2230.0001 1 g € 1000,00O

O ONH

SS

O

3

O

N N

O

O

N-[3-(o-Pyridyldisulfido)propanoyl]-15-amino-4,7,10,13-tetraoxa-pentade-canoyl succinimidyl ester FORMULA: C

23H

33N

3O

9S

2



PEG2235.0001 1 g € 1100,00O

O OHNH

SS

O

7

O

N

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-carboxy octa(ethylene glycol) FORMULA: C

27H

46N

2O

11S

2



PEG2240.0001 1 g € 1100,00O

O ONH

SS

O

7

O

N N

O

O

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-succinimidyl ester octa(ethylene glycol) FORMULA: C

31H

49N

3O

13S

2



PEG2245.0001 1 g € 1100,00O

O OHNH

SS

O

11

O

N

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-carboxy dodeca(ethylene glycol) FORMULA: C

35H

62N

2O

15S

2

MOLECULAR WEIGHT: 815 g/moleFURTHER INFORMATION: Spacer is 44 Atoms and 51.3 A


PEG2250.0001 1 g € 1100,00O

O ONH

SS

O

11

O

N N

O

O

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-succinimidyl ester dodeca(ethylene glycol) FORMULA: C

39H

65N

3O

17S

2


PEG3930 OPSS-dPEG™(16)-COOH PEG3930.0100 100 mg € 400,00

PEG3930.1000 1 g € 1400,00O

O OHNH

SS

O

15

O

N

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-(propionic acid) hexadeca(ethylene glycol) FORMULA: C

43H

78N

2O

19S

2


PEG3900 OPSS-dPEG™(16)-NHS PEG3900.0100 100 mg € 400,00

PEG3900.1000 1 g € 1400,00O

O ONH

SS

O

15

O

N N

O

O

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-(succinimidyl propionate) hexadeca(ethylene glycol) FORMULA: C

47H

81N

3O

21S

2



PEG3940.1000 1 g € 1400,00O

O OHNH

SS

O

19

O

N

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-(propionic acid) 20(ethylene glycol) FORMULA: C

51H

94N

2O

23S

2







PEG3910.1000 1 g € 1400,00O

O ONH

SS

O

19

O

N N

O

O

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-(succinimidyl propionate) 20(ethylene glycol) FORMULA: C

55H

97N

3O

25S

2



PEG2255.0001 1 g € 1200,00O

O OHNH

SS

O

23

O

N

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-carboxy 24(ethy-lene glycol) FORMULA: C

59H

110N

2O

27S

2



PEG2260.0001 1 g € 1100,00O

O ONH

SS

O

23

O

N N

O

O

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-succinimidyl ester 24(ethylene glycol) FORMULA: C

63H

113N

3O

29S

2



PEG3950.1000 1 g € 1500,00O

O OHNH

SS

O

35

O

N

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-(propionic acid) 36(ethylene glycol) FORMULA: C

83H

158N

2O

39S

2

MOLECULAR WEIGHT: 1872,26 g/moleFURTHER INFORMATION: Spacer is 137.8 atoms and 115 A approx


PEG3920.1000 1 g € 1500,00O

O ONH

SS

O

35

O

N N

O

O

alpha-[3-(o-Pyridyldisulfido)propanoylamido]-omega-(succinimidyl propionate) 36(ethylene glycol) FORMULA: C

87H

161N

3O

41S

2


PEG1216 OPSS-PEG-NHS PEG1216.0500 500 mg € 510,00

PEG1216.0001 1 g € 925,00SS

OO

ON

N

O

O

O

n

alpha-Pyridyl-2-disulfid-omega-carboxy succinimidyl ester poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000


PEG1217.1000 1 g € 925,00SS

OO

ON

N

O

O

O

n

alpha-Pyridyl-2-disulfid-omega-carboxy succinimidyl ester poly(ethylene glycol) (PEG-MW 5.000 Dalton) MOLECULAR WEIGHT: 5000 Da


PEG1215.1000 1 g € 925,00SS

OO

ON

N

O

O

O

n



PEG4720.1000 1 g € 925,00

SS

OO

ON

N

O

O

O

n



SS

OO

ON

N

O

O

O

n

Reference:

Basic Studies on Heterobifunctional Biotin-PEG Conjugates with a 3-4-Pyridyldithiopropionyl Marker on the second Terminus K.Kaiser M.Marek T.Hselgrbler H.Schindler H.J.Gruber Bioconjugate Chem. 1997; 8: 545-551.




3.7.3 Amino- and hydrazido-PeG-thiols PEG1197 H2N-PEG-SH*HCl PEG1197.0500 500 mg € 325,00

PEG1197.0001 1 g € 575,00H2N

OO

SH

n

alpha-Amino-omega-mercapto poly(ethylene glycol) hydrochloride (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da

PEG1198 H2N-PEG-SH*HCl PEG1198.0500 500 mg € 325,00

PEG1198.0001 1 g € 575,00H2N

OO

SH

n


PEG1196 H2N-PEG-SH*HCl PEG1196.0500 500 mg € 360,00

PEG1196.0001 1 g € 630,00H2NO

OSH

n


PEG1027 H2N-PEG-STrt PEG1027.0500 500 mg € 500,00

PEG1027.0001 1 g € 900,00alpha-Amino-omega-tritylthio poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da






PEG1114 Boc-NH-PEG-SH PEG1114.0500 500 mg € 275,00

PEG1114.0001 1 g € 450,00

NH

OO

SH

nO

Oalpha-t-Butyloxycarbonylamino-omega-mercapto poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG1115.0001 1 g € 450,00

NH

OO

SH

nO



PEG1113.0001 1 g € 500,00

NH

OO

SH

nO


H2NO

OSH

n

H2NO

NH

n

O

S

NH

OO

SH

nO

O




PEG1102 HS-PEG-CONH-NH-Boc PEG1102.0500 500 mg € 590,00

PEG1102.0001 1 g € 1050,00

HSO

NH

HN

NH

On

O

O

Oalpha-Thio-omega-t-butyloxycarbonyl-hydrazido poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG1103.0001 1 g € 1050,00

HSO

NH

HN

NH

On

O

O



PEG1101.0001 1 g € 1100,00

HSO

NH

HN

NH

On

O

O



HSO

NH

HN

NH

On

O

O

O

H2NOH

O

H2NOH

O

N

H2NOH

O

H2N NH2N

NH2

NH2 N

H2N NH2

OHO

N

NH2

NH2

OHO

N

H2N NH2

OH

O

O

N

H2N NH2

OH

O

O

O

N

NH2

NH2

OH

O

N

NH2

NH2

ArginineAmidino-GlycineBAA6380

Amino-guanidinopropionic acid

FAA1772

4-(guanidino)methylcyclohexane carboxylic acid

BAA1790

4-(guanidino)cyclohexanecarboxylic acid

BAA6380

2-(2-(amidino)ethoxy)acetic acid

BAA6070

Amino-guanidinobutyric acid

FAA6160

2-(2-(2-(amidino)ethoxy)ethoxy)acetic acid

BAA6080






3.7.4 Methoxy-PeG-thiolsMethoxy-PEG-thiols are reactive with metal surfaces, other thiols, disulfides, maleimides, vinyl sulfones, and halo-acetamides and incorporate properties as hydrophilicity and non-immunogenicity.

Product is highly soluble in water, methylene chloride and ethyl acetate, as well as other common organic solvents. Product is not soluble in methyl tertbutyl ether or hex-anes.

Hydrophilic capping agent for gold and silver surfaces.

Product handling and stability:Keep product under an inert atmosphere (dry nitrogen or argon recommended) to prevent oxidation to the disul-fide! If oxidized to the disulfide, product can be reduced in water or aqueous buffer using TCEP.

Reference:



10: 0-12-370501-0).

PEG3470 MeO-dPEG™(4)-SH PEG3470.0100 100 mg € 275,00

PEG3470.1000 1 g € 750,00O

OSH

OMeO

alpha-Methoxy-omega-mercapto tetra(ethylene glycol) FORMULA: C

9H

20O

4S


PEG1167 MeO-PEG(7)-SH PEG1167.0001 1 g € 350,00

PEG1167.0005 5 g € 1100,00MeO

SH

7

alpha-Methoxy-omega-mercapto hepta(ethylene glycol) FORMULA: C

15H

32O

7S


PEG1195 MeO-PEG(7)-SS-PEG(7)-OMe PEG1195.0001 1 g € 300,00

PEG1195.0005 5 g € 1050,00Me

OS

7

MeO

S

7

Methoxy-hepta(ethylen glycol)-disulfid FORMULA: C

30H

62O

14S

2



PEG3480.1000 1 g € 1000,00MeOO

SH

7

alpha-Methoxy-omega-mercapto octa(ethylene glycol) FORMULA: C

17H

36O

8S



PEG3490.1000 1 g € 1150,00MeOO

SH

11

alpha-Methoxy-omega-mercapto dodeca(ethylene glycol) FORMULA: C

25H

52O

12S






PEG1172 MeO-PEG-SH PEG1172.0001 1 g € 310,00

PEG1172.0005 5 g € 900,00

MeOO

OSH

n

alpha-Methoxy-omega-mercapto poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 Da


PEG1169.0005 5 g € 750,00

MeOO

OSH

n

alpha-Methoxy-omega-mercapto poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1171.0005 5 g € 750,00

MeOO

OSH

n



PEG1168.0005 5 g € 750,00

MeOO

OSH

n



PEG1170.0005 5 g € 750,00

MeOO

OSH

n



MeOO

OSH

n

PEG4745 MeO-PEG-OPSS PEG4745.0500 500 mg € 425,00

PEG4745.1000 1 g € 1275,00

MeOO

OS

nS N

alpha-Methoxy-omega-pyridyl-2-disulfid poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 Da


PEG4750.1000 1 g € 1075,00

MeOO

OS

nS N

alpha-Methoxy-omega-pyridyl-2-disulfid poly(ethylene glycol) (PEG-MW 2000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG4755.1000 1 g € 1075,00

MeOO

OS

nS N

alpha-Methoxy-omega-pyridyl-2-disulfid poly(ethylene glycol) (PEG-MW 5.000 Dalton) MOLECULAR WEIGHT: 5000 Da


PEG4760.1000 1 g € 1075,00

MeOO

OS

nS N



PEG4765.1000 1 g € 1075,00

MeOO

OS

nS N


MeOO

OS

nS N

Reference:

f Basic Studies on Heterobifunctional Biotin-PEG Conjugates with

a 3-4-Pyridyldithiopropionyl Marker on the second Terminus

K.Kaiser M.Marek T.Hselgrbler H.Schindler H.J.Gruber Bioconju-

gate Chem. 1997; 8: 545-551.




PEG2095 Ac-S-TEG-OH PEG2095.0100 100 mg € 300,00

PEG2095.0001 1 g € 625,00

SO

OO

O

OH

S-Acetyl-mercapto-tetra(ethylene glycol), S-Acetyl-2-(2-(2-(2-mercaptoe-thoxy)ethoxy)ethoxy)ethanol FORMULA: C

10H

20O

5S


PEG2470 Ac-S-OEG-OH PEG2470.0100 100 mg € 400,00

PEG2470.0001 1 g € 600,00

SO

OH

O

7

S-Acetyl-mercapto-octa(ethylene glycol), S-Acetyl-23-mercapto-3,6,9,12,15,18,21-heptaoxatricosan-1-ol FORMULA: C

18H

36O

9S


PEG3790 Ac-S-dPEG™(12)-OH PEG3790.0100 100 mg € 325,00

PEG3790.1000 1 g € 850,00

SO

OH

O

11

alpha-Acethylthio-omega-hydroxy dodeca(ethylene glycol) FORMULA: C

26H

52O

13S



PEG3800.1000 1 g € 950,00

SO

OH

O

15

alpha-Acethylthio-omega-hydroxy hexadeca(ethylene glycol) FORMULA: C

34H

68O

17S



PEG3810.1000 1 g € 1000,00

SO

OH

O

19

alpha-Acethylthio-omega-hydroxy 20(ethylene glycol) FORMULA: C

42H

84O

21S


PEG2010 HS-FA-PEG(8)-OH PEG2010.0100 100 mg € 375,00

HN

OOH

7HS

O

alpha-(11-Mercapto-undecanoylamido)-omega-hydroxy octa(ethylene glycol) FORMULA: C

27H

55NO

9S


3.7.5 hydroxy-PeG-thiols

Mercapto-PEG derivatives react with thiol reactive agents e.g., maleimides, vinyl sulfones or α-halo keto functional-ized reaction partners.

Highly hydrophilic, non-antigenic, non-immunogenic and non-toxic.





PEG1018 HO-PEG-SH PEG1018.0500 500 mg € 375,00

PEG1018.0001 1 g € 600,00

HOO

NH

n

O

SH

alpha-Hydroxy-omega-mercapto poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1019.0001 1 g € 600,00

HOO

NH

n

O

SH



PEG1017.0001 1 g € 650,00

HOO

NH

n

O

SH



PEG1024 HO-PEG-STrt PEG1024.0500 500 mg € 140,00

PEG1024.0001 1 g € 240,00HO

ONH

n

O

S

alpha-Hydroxy-omega-tritylthio poly(ethylene glycol) (PEG-MW 3.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 3000 DaFURTHER INFORMATION: -


PEG1025.0001 1 g € 240,00HO

ONH

n

O

S



PEG1023.0001 1 g € 300,00HO

ONH

n

O

S


HOO

NH

n

O

SH

HOO

NH

n

O

S





3.7.6 Bis-Mercapto-PeGPEG1122 HS-PEG-SH PEG1122.0001 1 g € 275,00

PEG1122.0005 5 g € 750,00

HSO

OSH

n

alpha,omega-Bis-mercapto poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da

PEG1124 HS-PEG-SH PEG1124.0001 1 g € 275,00

PEG1124.0005 5 g € 750,00

HSO

OSH

n


PEG1125 HS-PEG-SH PEG1125.0001 1 g € 275,00

PEG1125.0005 5 g € 750,00

HSO

OSH

n


PEG1121 HS-PEG-SH PEG1121.0001 1 g € 275,00

PEG1121.0005 5 g € 750,00

HSO

OSH

n


PEG1123 HS-PEG-SH PEG1123.0001 1 g € 275,00

PEG1123.0005 5 g € 750,00

HSO

OSH

n


PEG4715 OPSS-PEG-OPSS PEG4715.0500 500 mg € 350,00

PEG4715.1000 1 g € 1075,00

SO

OS

nS

SNN

alpha,omega-Bis(pyridyl-2-disulfid) poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG4725.1000 1 g € 1075,00

SO

OS

nS

SNN



PEG4730.1000 1 g € 1075,00

SO

OS

nS

SNN



PEG4735.1000 1 g € 1075,00

SO

OS

nS

SNN



PEG4740.1000 1 g € 1075,00

SO

OS

nS

SNN



SO

OS

nS

SNN

HSO

OSH

n




3.8 PeG-Maleinimides3.8.1 Non-PeG Maleinimido-Acid-crosslinkers PEG2135 mal-COOH PEG2135.0100 100 mg € 250,00

PEG2135.0001 1 g € 450,00N OH

O

O

O

3-(Maleinimido-1-yl)propanoic acid CAS-NO: 7423-55-4 FORMULA: C

7H

7NO

4


MAA1020 Mal-beta-Ala-OSu MAA1020.0001 1 g € 150,00

MAA1020.0005 5 g € 450,00

O

O

NN

O

O

O

O

3-(Maleimido)propionic acid N-succinimidyl ester, N-Maleoyl-beta-alanine N‘-hydroxysuccinimide ester CAS-NO: 55750-62-4 FORMULA: C

11H

10N

2O

6


PEG2090 MBS PEG2090.0100 100 mg € 275,00

PEG2090.0001 1 g € 550,00N

O

O

N

O

O

O

O

3-(Maleinimido-1-yl)benzoic acid N-hydroxy-succinimidyl ester CAS-NO: 58626-38-3 FORMULA: C

15H

10N

2O

6


MAA5400 Mal-AMCHC-OH MAA5400.0001 1 g € 100,00

MAA5400.0005 5 g € 400,00

MAA5400.0025 25 g € 1600,00

O

OHNO

O

trans-4-(maleimidomethyl)cyclohexane-1-carboxylic acid CAS-NO: 69907-67-1 FORMULA: C

12H

15NO

4


MAA1000 Mal-AMCHC-OSu MAA1000.0001 1 g € 180,00

MAA1000.0005 5 g € 720,00

O

O N

O

O

NO

Otrans-N-Succinimidyl 4-(maleimidomethyl)cyclohexane-1-carboxylate CAS-NO: 64987-85-5 FORMULA: C

16H

18N

2O

6



Application:A heterobifunctional cross-linking reagent with amine and thiol reactivity. Useful for preparation of enzyme immu-noconjugates and hapten carrier molecule conjugates. Contains 9 atom linker. An extended aliphatic spacer stabilizes the maleimide prior to coupling compared to aromatic spacers.

1. This reagent couples to molecules containing primary amine by amide bond formation in buffered solution at pH 7.5 6.5-8.5.

2. The second coupling to thiol containing molecules by forming thioether linkage is carried out at pH 6.8 6.5-7.0.




PEG1555 mal-EG(2)-COOH PEG1555.0100 100 mg € 275,00

PEG1555.0001 1 g € 775,00HN

OO OH

OO

N

O

O

3-(2-(2-(3-Maleinimidopropanamido)ethoxy)ethoxy)propanoic acid FORMULA: C

14H

20N

2O

7


PEG1560 mal-EG(2)-NHS PEG1560.0100 100 mg € 275,00

PEG1560.0001 1 g € 850,00HN

OO O

OO

N

O

O

N

O

O

3-(2-(2-(3-Maleinimidopropanamido)ethoxy)ethoxy)propanoic acid succinimidyl ester FORMULA: C

18H

23N

3O

9


PEG1570 mal-dPEG™(4)-COOH PEG1570.0100 100 mg € 325,00

PEG1570.0001 1 g € 925,00

OHOO

HN

O

N

O

O 3 O

1-Maleinimido-3-oxo-7,10,13,16-tetraoxa-4-azanonadecan-19-oic acid FORMULA: C

18H

28N

2O

9


PEG1575 mal-dPEG™(4)-NHS PEG1575.0100 100 mg € 325,00

PEG1575.0001 1 g € 925,00O

OO

O

HN

O

O

O

N

O

O

N

O

O

1-Maleinimido-3-oxo-7,10,13,16-tetraoxa-4-azanonadecan-19-oic acid succinimidyl ester FORMULA: C

22H

31N

3O

11



PEG3850.1000 1 g € 1000,00N N

H

OO OH

O

O

O O

5

alpha-Maleinimido-hexa(ethylen glycol)-omega-propionic acid FORMULA: C

22H

36N

2O

11



3.8.2 Maleinimido-PeG-Acids The general application of this class of heterobifunctional PEG crosslinkers is the controlled and selective conjuga-tion of an amine containing target, which reacts first with the NHS ester and then subsequently with a sulfhydryl containing complementary target molecule. Many biologi-cal molecules contain both the amine function and the complementary compounds. Peptides, oligonucleotides or other biologicals, for example, can be terminated with thiols or have thiols designed into them, and vice versa.

These products are designed to activate carrier proteins for conjugating hapten, e.g., peptide, to a carrier, e.g., KLH, BSA, OVA, etc., in order to reduce or eliminate the antigenicity and specificity issues with conventional acti-vating crosslinkers, which are reflected in the properties of the resulting antibodies. Much higher functional load-

ings can be achieved due to the increased water solubility imparted by the PEGylating reagent to the carrier–hapten conjugate, with decreased immunogenicity towards cross-linker and carrier.

Recommended solvents are DMAC, DMF or DMSO to ensure complete solubilization and homogeneity of the crosslinker in the buffer system. If water or buffer is preferred, the stabilities of both NHS ester and maleimide need to be considered.

Reference:

f Greg T. Hermanson, Bioconjugate Techniques, 2nd Ed, Elsevier

Inc., Burlington, MA 01803, April, 2008 (ISBN-13: 978-0-12-370501-3;

ISBN-10: 0-12-370501-0), pp. 276-335 and 718-722; protocols: pp. 788:

hapten-carrier conjugation; pp. 871: liposome conjugation; pp. 883:

antibody liposome conjugation.





PEG1585.0001 1 g € 1000,00

N NH

OO O

NO

O

O O

O

O

5

25-Maleinimido-23-oxo-4,7,10,13,16,19-hexaoxa-22-azapentacosanoic acid succinimidyl ester FORMULA: C

26H

39N

3O

13



PEG1615.0001 1 g € 1000,00

OO

OO

HN

OO

OO OH

O

N

O

O

O

1-Maleinimido-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid FORMULA: C

26H

44N

2O

13



PEG1590.0001 1 g € 1050,00

N NH

OO O

NO

O

O O

O

O

7

1-Maleinimido-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid succinimidyl ester FORMULA: C

30H

47N

3O

15


PEG2125 mal-PEG(12)-COOH PEG2125.0100 100 mg € 350,00

PEG2125.0001 1 g € 1200,00

NH

OO OH

O

11

O

N

O

O

3-(2-(2-(3-(Maleinimido-1-yl)propanamido)ethoxy)ethoxy)propanoic acid FORMULA: C

34H

60N

2O

17



PEG1550.0001 1 g € 1050,00

N NH

OO O

O

O

O O

N

O

O11

1-Maleinimido-3-oxo-7,10,13,16,19,22,25,28,31,34,37,40-dode-caoxa-4-azatritetracontan-43-oic acid succinimidyl ester FORMULA: C

38H

63N

3O

19



PEG3860.1000 1 g € 1200,00N N

H

OO OH

O

O

O O

15

alpha-Maleinimido-hexadeca(ethylen glycol)-omega-propionic acid FORMULA: C

42H

76N

2O

21



PEG3830.1000 1 g € 1300,00

N NH

OO O

O

O

O O

N

O

O15

alpha-Maleinimido-omega-(succinimidyl propionate) hexadeca(ethylen glycol) FORMULA: C

46H

79N

3O

23



PEG3870.1000 1 g € 1250,00N N

H

OO OH

O

O

O O

19

alpha-Maleinimido-20(ethylen glycol)-omega-propionic acid FORMULA: C

50H

92N

2O

25



PEG3840.1000 1 g € 1300,00

N NH

OO O

O

O

O O

N

O

O19

alpha-Maleinimido-omega-(succinimidyl propionate) 20(ethylen glycol) FORMULA: C

54H

95N

3O

27







PEG1600.0001 1 g € 1150,00N N

HO

O OH

O

O

O O

23

alpha-Maleinimido-24(ethylen glycol-omega-propionic acid FORMULA: C

58H

108N

2O

29



PEG1565.0001 1 g € 1200,00

N NH

OO O

NO

O

O O

O

O

23

alpha-Maleinimido-24(ethylen glycol-omega-propionic acid succinimi-dyl ester FORMULA: C

62H

111N

3O

31


PEG1209 mal-PEG(27)-NHS PEG1209.0100 100 mg € 450,00

PEG1209.0001 1 g € 1500,00

N NH

OO O

O

O

O O

N

O

O27

alpha-Maleinimido-omega-carboxy succinimidyl ester 27(ethylene glycol) FORMULA: C

70H

127N

3O

35


PEG1059 mal-PEG-COOH PEG1059.0500 500 mg € 475,00

PEG1059.0001 1 g € 800,00N

HN

OO

O

OO

OH

On

alpha-Maleinimido-omega-carboxy poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG1060.0001 1 g € 800,00N

HN

OO

O

OO

OH

On



PEG1058.0001 1 g € 850,00N

HN

OO

O

OO

OH

On


PEG1062 mal-PEG-NHS PEG1062.0500 500 mg € 500,00

PEG1062.0001 1 g € 875,00

PEG1062.0005 5 g € 3500,00N

HN

OO

O

OO

ON

O

O

O

n

alpha-Maleinimido-omega-carboxy succinimidyl ester poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG1063.0001 1 g € 875,00N

HN

OO

O

OO

ON

O

O

O

n



PEG1061.0001 1 g € 950,00N

HN

OO

O

OO

ON

O

O

O

n



NHN

OO

O

OO

OH

On

NHN

OO

O

OO

ON

O

O

O

n




PEG2185 MBz-PEG(4)-COOH PEG2185.0100 100 mg € 350,00

PEG2185.0001 1 g € 925,00

OO

OO OH

O

NH

N

OO

O

N-[3-(Maleinimid-1-yl)-benzoxy]-15-amino-4,7,10,13-tetraoxa-pentadeca-noic acid FORMULA: C

22H

28N

2O

9


PEG2190 MBz-PEG(4)-NHS PEG2190.0100 100 mg € 350,00

PEG2190.0001 1 g € 925,00

OO

OO O

O

NH

N

OO

O

N

O

O

N-[3-(Maleinimid-1-yl)-benzoxy]-15-amino-4,7,10,13-tetraoxa-pentadeca-noyl succinimidyl ester FORMULA: C

26H

31N

3O

11



PEG2195.0001 1 g € 1050,00O

O OHNH

N

OO

O 7

Oalpha-N-[3-(Maleinimid-1-yl)-benzylamid]-omega-carboxy octa(ethylene glycol) FORMULA: C

30H

44N

2O

13



PEG2200.0001 1 g € 1050,00O

O ONH

N

OO

O 7

O

N

O

O

alpha-N-[3-(Maleinimid-1-yl)-benzylamid]-omega-succinimidyl ester octa(ethylene glycol) FORMULA: C

34H

47N

3O

15



PEG2205.0001 1 g € 1050,00O

O OHNH

N

OO

O 11

Oalpha-N-[3-(Maleinimid-1-yl)-benzylamid]-omega-carboxy dodeca(ethylene glycol) FORMULA: C

38H

60N

2O

17

MOLECULAR WEIGHT: 816,89 g/moleFURTHER INFORMATION: Spacer 47 atoms and 54.5 A


PEG2210.0001 1 g € 1050,00O

O ONH

N

OO

O 11

O

N

O

O

alpha-N-[3-(Maleinimid-1-yl)-benzylamid]-omega-succinimidyl ester dodeca(ethylene glycol) FORMULA: C

42H

63N

3O

19



PEG2215.0001 1 g € 1150,00O

O OHNH

N

OO

O 23

Oalpha-N-[3-(Maleinimid-1-yl)-benzylamid]-omega-carboxy 24(ethylene glycol) FORMULA: C

62H

108N

2O

29

MOLECULAR WEIGHT: 1345,52 g/moleFURTHER INFORMATION: Spacer is 83 atoms amd 96.8 A


PEG2220.0001 1 g € 1150,00O

O ONH

N

OO

O 23

O

N

O

O

alpha-N-[3-(Maleinimid-1-yl)-benzylamid]-omega-succinimidyl ester 24(ethylene glycol) FORMULA: C

66H

111N

3O

31






3.8.3 Maleinimido-PeG-Amines and hydrazides

The general application of this class of heterobifunctional PEG crosslinkers is the controlled and selective conjuga-tion of a carbonyl containing target, which reacts first with an aldehyde or ketone and then subsequently with a sulfhydryl containing complementary target molecule (such as a protein, peptide or modified oligonucleotide, which reacts with the maleimide).

The PEG containing heterobifunctional crosslinker incor-porates hydrophilicity, water solubility and nonimmuno-genicity.

The formed hydrazine in the conjugate is stable under neutral or basic pH, but will be hydrolyzed at acidic pH. This can, for example, be used to conjugate a drug or other similar species to a targeting carrier.

PEG2105 MP-EDA*TFA PEG2105.0100 100 mg € 375,00

PEG2105.0001 1 g € 775,00N N

H

O

NH3+

O

O

O

O-F

FF

2-(3-(Maleinimid-1-yl)propanamido)ethanaminium trifluoracetat FORMULA: C

9H

14N

3O

3*C

2F

3O

2


PEG1580 mal-dPEG™(4)-NHNH-Boc PEG1580.0100 100 mg € 325,00

PEG1580.0001 1 g € 850,00HNO

O

HN

O

N

O

O 3 O

NH

O

O1-Maleinimido-3-oxo-7,10,13,16-tetraoxa-4-azanonadecan-19-oyl-(N‘-t-butyloxycarbonyl)hydrazid FORMULA: C

23H

38N

4O

10



PEG3880.1000 1 g € 1000,00HNO

OHN

O

N

O

O 7 O

NH

O

Oalpha-Maleinimido-omega-(t-butyloxycarbonylhydrazidopropionate) octa(ethylen glycol) FORMULA: C

31H

54N

4O

14



PEG3890.1000 1 g € 1150,00HNO

OHN

O

N

O

O 11 O

NH

O

Oalpha-Maleinimido-omega-(t-butyloxycarbonylhydrazidopropionate) dodeca(ethylen glycol) FORMULA: C

39H

70N

4O

18


Protocol & References:



10: 0-12-370501-0); pp. 297-302.





PEG2375 MeO-PEG(4)-mal PEG2375.0100 100 mg € 325,00

PEG2375.0001 1 g € 700,00

OO

OMeO N

HN

O O

O

alpha-Methoxy-omega-maleinimido tetra(ethylene glycol) FORMULA: C

16H

26N

2O

7


PEG2380 MeO-PEG(8)-mal PEG2380.0100 100 mg € 350,00

PEG2380.0001 1 g € 850,00MeO

ONH

N

O O

O

7

alpha-Methoxy-omega-maleinimido octa(ethylene glycol) FORMULA: C

24H

42N

2O

11


PEG1665 MeO-dPEG™(12)-mal PEG1665.0100 100 mg € 375,00

PEG1665.0001 1 g € 1050,00

MeO

OHN

O

N

O

O11

Maleinimidyl-N-(2,5,8,11,14,17,20,23,26,29,32,35-dodecaoxaheptatria-contan-37-yl)propanamide FORMULA: C

32H

58N

2O

15



PEG1675.0001 1 g € 1350,00

MeO

OHN

O

N

O

O23

alpha-Methoxy-omega-maleinimidyl-propanamide 24(ethylene glycol) FORMULA: C

56H

106N

2O

27



PEG3360.1000 1 g € 1450,00

MeO

OHN

O

N

O

O35


80H

154N

2O

39



PEG3370.1000 1 g € 1550,00

MeO

OHN

O

N

O

O47


104H

202N

2O

51


3.8.4 Methoxy-PeG-Maleinimides

Sulfhydryl/thiol reactive PEGylation modifier, when incorporated into peptides (cysteine), proteins (site di-rected mutagenesis) or oligonucleotides (thiol modified), increases water solubility, stability, hydrodynamic volume, and decreases aggregation.


Reference:



10: 0-12-370501-0). pg. 30.





PEG1150 MeO-PEG-mal PEG1150.0001 1 g € 200,00

PEG1150.0005 5 g € 700,00

MeO

ON

n

O

O

alpha-Methoxy-omega-ethyl-maleinimide poly(ethylene glycol) (PEG-MW 750 Dalton) FORMULA: - MOLECULAR WEIGHT: 750 g/moleFURTHER INFORMATION: -


PEG1147.0005 5 g € 575,00

MeO

ON

n

O

O

alpha-Methoxy-omega-ethyl-maleinimide poly(ethylene glycol) (PEG-MW 2.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 2000 DaFURTHER INFORMATION: -


PEG1149.0005 5 g € 575,00

MeO

ON

n

O

O



PEG1146.0005 5 g € 675,00

MeO

ON

n

O

O



PEG1148.0005 5 g € 675,00

MeO

ON

n

O

O



MeO

ON

n

O

O

H2N (S)(S)OH

O

(R)(R)

OH

H2NOH

O

OH

H2NOH

O

OH

serine threonine 3-hydroxy-leucineHAA1650






3.8.5 Bis-Maleinimido-PeGs PEG1485 mal-dPEG™(3)-mal PEG1485.0050 50 mg € 300,00

PEG1485.0001 1 g € 775,00

HNO

ONH

2

N

O

O

O

O

N

O

O

Bis-(1,13-(3-maleinimidopropionyl)amido)-4,7,10-trioxatridecane FORMULA: C

24H

34N

4O

9


PEG2085 mal-PEG(12)-mal PEG2085.0050 50 mg € 375,00

PEG2085.0001 1 g € 1100,00

N NH

O

O

O

ONH

N

O O

O

11

alpha,omega-Bis-[(3-maleinimid-1-yl)propanoylamido] dodeca(ethylene glycol) FORMULA: C

38H

62N

4O

17


PEG1127 mal-PEG-mal PEG1127.0001 1 g € 175,00

PEG1127.0005 5 g € 575,00O

ON

n

O

ON

O

O

alpha,omega-Bis-maleinimido poly(ethylene glycol) (PEG-MW 2.000 Dalton) FORMULA: - MOLECULAR WEIGHT: 2000 DaFURTHER INFORMATION: -


PEG1129.0005 5 g € 575,00O

ON

n

O

ON

O

O



PEG1130.0005 5 g € 575,00O

ON

n

O

ON

O

O



PEG1126.0005 5 g € 575,00O

ON

n

O

ON

O

O



PEG1128.0005 5 g € 575,00O

ON

n

O

ON

O

O


Reference:



10: 0-12-370501-0); pp. 235-276 and 714-718.


OO

N

n

O

ON

O

O




PEG4790 MeO-PEG-Si(OMe)3 PEG4790.0500 500 mg € 175,00

PEG4790.1000 1 g € 325,00

MeOO

NH

NH

nSi(OMe)3

Oalpha-Methoxy-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG4795.1000 1 g € 325,00

MeOO

NH

NH

nSi(OMe)3



PEG4800.1000 1 g € 325,00

MeOO

NH

NH

nSi(OMe)3



PEG4805.1000 1 g € 325,00

MeOO

NH

NH

nSi(OMe)3



PEG4810.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3

OOalpha-Propargylacetamido-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG4815.1000 1 g € 900,00alpha-Propargylacetamido-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 5.000 Dalton) MOLECULAR WEIGHT: 5000 Da

3.9 PeG-SilanesPeG-Silanes for modification of silicate surfaces.

OSi

O

O

O

O

NH

OSi

O

O

O

O

O

Si

O

O

O

O

NH

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

OSi

O

O

O

O

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

O

Si

O

O

O

O

O

Si

O

O

O

O

NH

OSi

O

O

O

O

NH

HO

HOHO

HOHO HO HO

HO

HO

HO

HO

HO

HOHO

HOHO

HOHO

HOOH

HO

HO

HOHO HO

HO

O

O

OO

O

O

O


NH

ONH

NH

nSi(OMe)3

OO

MeOO

NH

NH

nSi(OMe)3

O









PEG4830.1000 1 g € 900,00N3

ONH

NH

nSi(OMe)3

Oalpha-Azido-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG4835.1000 1 g € 900,00alpha-Azido-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 5.000 Dalton) MOLECULAR WEIGHT: 5000 Da






NH

ONH

NH

nSi(OMe)3

OO

N3O

NH

NH

nSi(OMe)3

O


PEG4850.1000 1 g € 900,00

NH

ONH

NH

nSi(OMe)3

OO

S

NH

HN

Oalpha-Biotinyl-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 3.000 Dalton) MOLECULAR WEIGHT: 3000 Da


PEG4855.1000 1 g € 900,00alpha-Biotinyl-omega-trimethoxysilyl poly(ethylene glycol) (PEG-MW 5.000 Dalton) MOLECULAR WEIGHT: 5000 Da





NH

ONH

NH

nSi(OMe)3

OO

S

NH

HN

O




PEG1076 Br-PEG-Br PEG1076.0001 1 g € 75,00

PEG1076.0005 5 g € 275,00O

OBr

nBr

alpha,omega-Bis-bromo poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da

PEG1078 Br-PEG-Br PEG1078.0001 1 g € 75,00

PEG1078.0005 5 g € 275,00O

OBr

nBr


PEG1079 Br-PEG-Br PEG1079.0001 1 g € 75,00

PEG1079.0005 5 g € 275,00O

OBr

nBr


PEG1075 Br-PEG-Br PEG1075.0001 1 g € 75,00

PEG1075.0005 5 g € 275,00O

OBr

nBr


PEG1077 Br-PEG-Br PEG1077.0001 1 g € 75,00

PEG1077.0005 5 g € 275,00O

OBr

nBr


PEG1135 MeO-PEG-Br PEG1135.0001 1 g € 90,00

PEG1135.0005 5 g € 350,00MeO

OBr

n

alpha-Methoxy-omega-bromo poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 g/mole


PEG1132.0005 5 g € 275,00MeO

OBr

n

alpha-Methoxy-omega-bromo poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1134.0005 5 g € 275,00MeO

OBr

n



PEG1131.0005 5 g € 350,00MeO

OBr

n



PEG1133.0005 5 g € 350,00MeO

OBr

n


3.10 other PeG Reagents3.10.1 Bromo-PeGs


OO

Br

nBr

MeOO

Br

n




PEG1016 HO-PEG(8)-OH PEG1016.0005 5 g € 250,00

PEG1016.0025 25 g € 750,00O

OOH

6HO

Octa-ethylene glycol CAS-NO: 5117-19-1 FORMULA: C

16H

34O

9


PEG1015 HO-PEG(12)-OH PEG1015.0005 5 g € 350,00

PEG1015.0025 25 g € 1100,00O

OOH

10HO

Dodeca-ethylene glycol CAS-NO: 6790-09-6 FORMULA: C

24H

50O

13


PEG1009 HO-PEG(28)-OH PEG1009.0001 1 g € 200,00

PEG1009.0005 5 g € 575,00O

OOH

26HO

alpha,omega-Bis-hydroxy 28(ethylene glycol) FORMULA: C

56H

114O

29


3.10.2 Bishydroxy-PeGs Article No. Quantity Price

PEG1011 HO-PEG-OH PEG1011.0005 5 g € 60,00

PEG1011.0025 25 g € 150,00O

OOH

nHO

alpha,omega-Bis-hydroxy poly(ethylene glycol) (PEG-MW 2.000 Dalton) CAS-NO: 25322-68-3 MOLECULAR WEIGHT: 2000 Da

PEG1013 HO-PEG-OH PEG1013.0005 5 g € 60,00

PEG1013.0025 25 g € 150,00O

OOH

nHO


PEG1014 HO-PEG-OH PEG1014.0005 5 g € 60,00

PEG1014.0025 25 g € 150,00O

OOH

nHO


PEG1010 HO-PEG-OH PEG1010.0005 5 g € 60,00

PEG1010.0025 25 g € 150,00O

OOH

nHO


PEG1012 HO-PEG-OH PEG1012.0005 5 g € 60,00

PEG1012.0025 25 g € 150,00O

OOH

nHO


OO

OH

nHO




PEG1720 MeO-EG(2)-Tos PEG1720.0001 1 g € 350,00

OO

OS

O O

Me2-(2-Methoxyethoxy)ethyl 4-methylbenzenesulfonate FORMULA: C

12H

18O

5S


PEG2155 MeO-PEG(4)-OH PEG2155.0100 100 mg € 300,00

PEG2155.0001 1 g € 425,00

OO

OO OH

2,5,8,11-Tetraoxatridecan-13-ol FORMULA: C

9H

20O

5


PEG1695 MeO-dPEG™(4)-Tos PEG1695.0001 1 g € 400,00

MeO

OS

O O

Me

4

2,5,8,11-Tetraoxatridecan-13-yl 4-methylbenzenesulfonate FORMULA: C

16H

26O

7S


PEG1032 MeO-PEG(7)-OH PEG1032.0001 1 g € 350,00

PEG1032.0005 5 g € 650,00MeOO

OH

6

Hepta(ethylene glycol) methylether CAS-NO: 4437-01-8 FORMULA: C

15H

32O

8


PEG3820 MeO-dPEG™(7)-Tos PEG3820.1000 1 g € 550,00

MeO

OS

O O

Me

7

alpha-Methoxy-omega-tosyl hepta(ethylene glycol) FORMULA: C

22H

38O

10S


PEG1038 MeO-PEG(11)-OH PEG1038.0001 1 g € 425,00

PEG1038.0005 5 g € 800,00MeOO

OH

10

Undecae(ethylene glycol) methylether CAS-NO: 114740-40-8 FORMULA: C

23H

48O

12


3.10.3 Methoxy-PeG-Alcohols

Useful intermediates to design other reactive PEG species. The hydroxyl function can be derivatized to a variety of other functionalities. Potential PEGylation applications for this reagent include:

1. surface modification;

2. increasing solubility;

3. blocking/capping.

Will reduce or eliminate non-specific interactions and aggregation. Reduces immunogenicity and increases water solubility.





PEG3250 MeO-dPEG™(15)-OH PEG3250.0100 100 mg € 275,00

PEG3250.1000 1 g € 450,00MeOO

OH

14

Pentadecae(ethylene glycol) methylether FORMULA: C

31H

64O

16



PEG3260.1000 1 g € 600,00MeOO

OH

18

Nonadecae(ethylene glycol) methylether FORMULA: C

39H

80O

20



PEG3270.1000 1 g € 650,00MeOO

OH

22

alpha-Methoxy-omega-hydroxy-23(ethylen glycol) FORMULA: C

47H

96O

24



PEG3280.1000 1 g € 1000,00MeOO

OH

35

alpha-Methoxy-omega-hydroxy-36(ethylen glycol) FORMULA: C

73H

148O

37



PEG1037 MeO-PEG-OH PEG1037.0005 5 g € 60,00

PEG1037.0025 25 g € 150,00MeOO

OH

n

alpha-Methoxy-omega-hydroxy poly(ethylene glycol) (PEG-MW 750 Dalton) CAS-NO: 9004-74-4 MOLECULAR WEIGHT: 750 Da


PEG1034.0025 25 g € 150,00MeOO

OH

n

alpha-Methoxy-omega-hydroxy poly(ethylene glycol) (PEG-MW 2.000 Dalton) CAS-NO: 9004-74-4 MOLECULAR WEIGHT: 2000 Da


PEG1036.0025 25 g € 150,00MeOO

OH

n



PEG1033.0005 5 g € 350,00MeOO

OH

n



PEG1035.0005 5 g € 350,00MeOO

OH

n


PEG1218 MeO-PEG-OMs PEG1218.0001 1 g € 75,00

PEG1218.0005 5 g € 300,00MeOO

O

nS

Me

O O

alpha-Methoxy-omega-mesitylate poly(ethylene glycol) (PEG-MW 5.000 Dalton) MOLECULAR WEIGHT: 5000 Da

MeOO

OH

n




PEG2170 MeO-PEG(4)-CHO PEG2170.0100 100 mg € 250,00

PEG2170.0001 1 g € 650,00

OO

OO

H

Oalpha-Methoxy-omega-propanal tetra(ethylene glycol) FORMULA: C

10H

20O

5



PEG2175.0001 1 g € 650,00O

O H7

Oalpha-Methoxy-omega-propanal octa(ethylene glycol) FORMULA: C

18H

36O

9


PEG2335 MeO-PEG(11)-PrCHO PEG2335.0100 100 mg € 300,00

PEG2335.0001 1 g € 950,00O

OMe11

H

Oalpha-Methoxy-omega-propional undeca(ethylene glycol) FORMULA: C

26H

52O

13



PEG2180.0001 1 g € 1250,00O

O H23

Oalpha-Methoxy-omega-propanal 24(ethylene glycol) FORMULA: C

50H

100O

25


3.10.4 PeG-AldehydesAmine and hydrazide reactive PEGylating reagent usually converted to a secondary amine via reductive amination protocols.


Highly water soluble, non-immunogenic, reduces aggrega-tion and toxicity.

H

NH2 +PEG

O

NH

PEG

+ NaCNBH3

References:



10: 0-12-370501-0). pp. 200-202: general discussion on reactions

with hydrazides, reductive amination, and the Mannich condensa-

tion; pp. 232: protocol for reductive amination with proteins.

f Nucleophilic Catalysis of Oxime Ligation, Anouk Dirksen, Tilman M.

Hackeng, and Philip E. Dawson; Angew. Chem. Int. Ed. 2006; 45: 7581-7584.

f Rapid Oxime and Hydrazone Ligations with Aromatic Aldehydes

for Biomolecular Labeling; Anouk Dirksen and Philip E. Dawson;

Bioconjugate Chem. 2008; 19: 2543-2548.

f Nucleophilic Catalysis of Hydrazone Formation and Transimina-

tion: Implications for Dynamic Covalent Chemistry, Anouk Dirksen,

Sjoerd Dirksen, Tilman M. Hackeng, and Philip E. Dawson; J. Am.

Chem. Soc. 2006; 128: 15602-15603.

f High-efficiency labeling of sialylated glycoproteins on living cells,

Ying Zeng, T N C Ramya, Anouk Dirksen, Philip E Dawson, James C

Paulson; Nature Methods 2009; 6(3): 207-209.

f A.F. Abedel-Magid, et al.; J. Org. Chem. 1996; 61: 3849-3862.

f H. D. King, et al.; Bioconjugate Chem. 1999; 10: 279-288.

f A. Kale; V. P. Torchilin, et al.; Bioconjugate Chem. 2007; 18: 363-370.

f R.M. Sawant, et al.; Bioconjugate Chem. 2006; 17: 943-949.

f H. Gaertner, et al.; Bioconjugate Chem. 2008; 19: 480-489.

f P. R. Hamann, et al.; Bioconjugate Chem. 2002; 13: 47-58.

f Y. Bae, et al.; Bioconjugate Chem. 2007; 18: 1131-1139.

f T. R. Smith, et al.; Bioconjugate Chem. 2007; 18: 1355-1359.

f C. Lee, et al.; Bioconjugate Chem. 2006; 17: 1364-1368.




PEG1145 MeO-PEG-CHO PEG1145.0001 1 g € 275,00

PEG1145.0005 5 g € 675,00MeO

O

HN

n O

H

Oalpha-Methoxy-omega-formyl poly(ethylene glycol) (PEG-MW 750 Dalton) MOLECULAR WEIGHT: 750 g/mole


PEG1142.0005 5 g € 450,00MeO

O

HN

n O

H

Oalpha-Methoxy-omega-formyl poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1144.0005 5 g € 450,00MeO

O

HN

n O

H



PEG1141.0005 5 g € 575,00MeO

O

HN

n O

H



PEG1143.0005 5 g € 575,00MeO

O

HN

n O

H



MeOO

HN

n O

H

O

PEG1179 OHC-PEG-CHO PEG1179.0001 1 g € 200,00

PEG1179.0005 5 g € 450,00HN

O

HN

n O

H

O

H

O

Oalpha,omega-Bis-formyl poly(ethylene glycol) (PEG-MW 2.000 Dalton) MOLECULAR WEIGHT: 2000 Da


PEG1181.0005 5 g € 450,00HN

O

HN

n O

H

O

H

O



PEG1182.0005 5 g € 450,00HN

O

HN

n O

H

O

H

O



PEG1178.0005 5 g € 450,00HN

O

HN

n O

H

O

H

O



PEG1180.0005 5 g € 450,00HN

O

HN

n O

H

O

H

O


HN

O

HN

n O

H

O

H

O

O





DDN2000 PEG-Pentrimer-G1-(NH2+4xBoc-NH)

DDN2000.0001 1 g € 875,00

NN

N

O

O OO O

NH

O

O

O

NHBoc

HN

O

O

O

BocHN

NH

O

O

O

BocHN

HN

O

O

O

NHBoc

NH

O

O

O

NH2

Pentavalent PEG based Dendrimer-Generation-1 with one amino and four t-butyloxycarbonylamino functions, purity 99% FORMULA: C

84H

165N

13O

28


DDN2010 PEG-Pentrimer-G1-(Z-NH+4xBoc-NH)

DDN2010.0001 1 g € 875,00

NN

N

O

O OO O

NH

O

O

O

NHBoc

HN

O

O

O

BocHN

NH

O

O

O

BocHN

HN

O

O

O

NHBoc

NH

O

O

O

NHCbz

Pentavalent PEG based Dendrimer-Generation-1 with one benzyloxycar-bonylamino and four t-butyloxycarbonylamino functions, purity 99% FORMULA: C

92H

171N

13O

30


DDN2020 PEG-Pentrimer-G1-(TFA-NH+4xBoc-NH)

DDN2020.0001 1 g € 875,00

NN

N

O

O OO O

NH

O

O

O

NHBoc

HN

O

O

O

BocHN

NH

O

O

O

BocHN

HN

O

O

O

NHBoc

NH

O

O

O

NHTFA

Pentavalent PEG based Dendrimer-Generation-1 with one trifluoroacet-amido and four t-butyloxycarbonylamino functions, purity 99% FORMULA: C

86H

164F

3N

13O

29


DDN2030 PEG-Pentrimer-G1-(N3+4xBoc-NH)

DDN2030.0001 1 g € 875,00

NN

N

O

O OO O

NH

O

O

O

NHBoc

HN

O

O

O

BocHN

NH

O

O

O

BocHN

HN

O

O

O

NHBoc

NH

O

O

O

N3

Pentavalent PEG based Dendrimer-Generation-1 with one azido and four t-butyloxycarbonylamino functions, purity 99% FORMULA: C

84H

163N

15O

28


4. Available Dendrimers and Dendron Building Blocks4.1 Available PeG based Dendrimers

Derivatives with different functional groups and of higher generation are in development

and will soon be available. Please inquire for the Pentrimers of your choice!




DDN2040 PEG-Pentrimer-G1-(N3+4xNH2)

DDN2040.0001 1 g € 875,00

NN

N

O

O OO O

NH

O

O

O

NH2

HN

O

O

O

H2N

NH

O

O

O

H2N

HN

O

O

O

NH2

NH

O

O

O

N3

Pentavalent PEG based Dendrimer-Generation-1 with one azido and four amino functions, purity 99% FORMULA: C

64H

131N

15O

20


DDN2050 PEG-Pentrimer-G1-(NH2+4xN3)

DDN2050.0001 1 g € 990,00

NN

N

O

O OO O

NH

O

O

O

N3

HN

O

O

O

N3

NH

O

O

O

N3

HN

O

O

O

N3

NH

O

O

O

NH2

Pentavalent PEG based Dendrimer-Generation-1 with one amino and four azido functions, purity 99% FORMULA: C

64H

125N

21O

20


DDN2060 PEG-Pentrimer-G1-(Boc-NH+4xN3)

DDN2060.0001 1 g € 990,00

NN

N

O

O OO O

NH

O

O

O

N3

HN

O

O

O

N3

NH

O

O

O

N3

HN

O

O

O

N3

NH

O

O

O

NHBoc

Pentavalent PEG based Dendrimer-Generation-1 with one t-butyloxycar-bonylamino and four azido functions, purity 99% FORMULA: C

69H

133N

21O

22


Need other pattern

or functional groups?

The following combinations

are available on request:

1x Aloc-NH 4x Boc-NH

1x Boc-NH 4x TFA-NH

1x Boc-NH 4x Aloc-NH

Inquire for any other

functional group pattern!

Need PEG spacers with different length?

Please inquire for the Dendrimer of your choice.




DDN1000 Azido-Dendron-G1-(OH)2

DDN1000.0500 500 mg € 300,00

DDN1000.1000 1 g € 510,00

DDN1000.5000 5 g € 2260,00

OH

OH

O

O

N3

Azidohexyl-Dendron-Generation-1-dihydroxide, 6-Azidohexyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate FORMULA: C

11H

21N

3O

4


DDN1050 Azido-Dendron-G1-Acetonide DDN1050.0500 500 mg € 260,00

DDN1050.1000 1 g € 440,00

DDN1050.5000 5 g € 1960,00O

O

O

O

N3Azidohexyl-Dendron-Generation-1-acetonide, 6-Azidohexyl 2,2,5-trime-thyl-1,3-dioxane-5-carboxylate FORMULA: C

14H

25N

3O

4


DDN1010 Azido-Dendron-G2-(OH)4 DDN1010.0500 500 mg € 370,00

DDN1010.1000 1 g € 640,00

DDN1010.5000 5 g € 2860,00

OH

OH

O

O

OH

OH

O

O

O

O

N3

Azidohexyl-Dendron-Generation-2-tetrahydroxide, 2-((6-azidohexyloxy)carbonyl)-2-methylpropane-1,3-diyl bis(3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate) FORMULA: C

21H

37N

3O

10


DDN1060 Azido-Dendron-G2-(Acetonide)2 DDN1060.0500 500 mg € 340,00

DDN1060.1000 1 g € 570,00

DDN1060.5000 5 g € 2570,00

O

O

O

O

O

O

O

O

O

O

N3

Azidohexyl-Dendron-Generation-2-diacetonide, 2-((6-azidohexyloxy)carbonyl)-2-methylpropane-1,3-diyl bis(2,2,5-trimethyl-1,3-dioxane-5-carboxylate) FORMULA: C

27H

45N

3O

10


4.2 Available 2,2-bis(hydroxymethyl) propionic acid based Dendrons

4.2.1 Azido Dendrons Article No. Quantity Price

First generation pentavalent PEG based dendrimer with three different reactive groups, for example Click reacti-ve, carboxylic acid (amine reactive) and protected amine (nucleophilic).

Second generation dendrimer based on a pentavalent PEG based building block for sophisticated applications in drug delivery, diagnostics, combination therapy or perso-nalized medicine.





DDN1020.1000 1 g € 780,00

DDN1020.5000 5 g € 3520,00

HO HO

OO

OH

OH

O

O

O

O

HO HO

OO

OH

OH

O

O

O

O

O

O

N3

Azidohexyl-Dendron-Generation-3-octahydroxide FORMULA: C

41H

69N

3O

22



DDN1070.1000 1 g € 710,00

DDN1070.5000 5 g € 3230,00

O

O

O

O

OO

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

N3

Azidohexyl-Dendron-Generation-3-tetraacetonide FORMULA: C

53H

85N

3O

22



DDN1030.0500 500 mg € 630,00

DDN1030.1000 1 g € 1110,00

Azidohexyl-Dendron-Generation-4-hexadecihydroxide FORMULA: C

81H

133N

3O

46



DDN1080.0500 500 mg € 560,00

DDN1080.1000 1 g € 980,00

Azidohexyl-Dendron-Generation-4-octaacetonide FORMULA: C

105H

165N

3O

46



DDN1040.0500 500 mg € 790,00

DDN1040.1000 1 g € 1380,00

Azidohexyl-Dendron-Generation-5-dotriacontahydroxide FORMULA: C

161H

261N

3O

94



DDN1090.0500 500 mg € 710,00

DDN1090.1000 1 g € 1250,00

Azidohexyl-Dendron-Generation-5-hexadeciacetonide FORMULA: C

209H

325N

3O

94






4.2.2 Alkyne DendronsDDN1100 Alkynyl-Dendron-G1-(OH)2 DDN1100.0500 500 mg € 230,00

DDN1100.1000 1 g € 370,00

DDN1100.5000 5 g € 1620,00OH

OH

O

OPropynyl-Dendron-Generation-1-dihydroxide, Prop-2-ynyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate FORMULA: C

8H

12O

4


DDN1150 Alkynyl-Dendron-G1-Acetonide DDN1150.0500 500 mg € 190,00

DDN1150.1000 1 g € 310,00

DDN1150.5000 5 g € 1300,00O

O

O

OPropynyl-Dendron-Generation-1-acetonide, Prop-2-ynyl 2,2,5-trime-thyl-1,3-dioxane-5-carboxylate FORMULA: C

11H

16O

4


DDN1110 Alkynyl-Dendron-G2-(OH)4 DDN1110.0500 500 mg € 300,00

DDN1110.1000 1 g € 510,00

DDN1110.5000 5 g € 2280,00

OH

OH

O

O

OH

OH

O

O

O

OPropynyl-Dendron-Generation-2-tetrahydroxide, 2-Methyl-2-((prop-2-ynyloxy)carbonyl)propane-1,3-diyl bis(3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate) FORMULA: C

18H

28O

10


DDN1160 Alkynyl-Dendron-G2-(Acetonide)2 DDN1160.0500 500 mg € 260,00

DDN1160.1000 1 g € 430,00

DDN1160.5000 5 g € 1900,00O

O

O

O

O

O

O

O

O

OPropynyl-Dendron-Generation-2-diacetonide, 2-Methyl-2-((prop-2-ynyloxy)carbonyl)propane-1,3-diyl bis(2,2,5-trimethyl-1,3-dioxane-5-carboxylate) FORMULA: C

24H

36O

10



DDN1120.1000 1 g € 640,00

DDN1120.5000 5 g € 2880,00

HO HO

OO

OH

OH

O

O

O

O

HO HO

OO

OH

OH

O

O

O

O

O

O

Propynyl-Dendron-Generation-3-octahydroxide FORMULA: C

38H

60O

22



DDN1170.1000 1 g € 570,00

DDN1170.5000 5 g € 2550,00

O

O

O

O

OO

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

Propynyl-Dendron-Generation-3-tetraacetonide FORMULA: C

50H

76O

22



DDN1130.0500 500 mg € 560,00

DDN1130.1000 1 g € 980,00

OH

OH

OH

OH

OH

OH

OH

OH

OHOH

OHOH

HOHO

HOHO

OO O O

OO

O

O

O

O

O

O

O

O

OO O O

OO

O

O

O

O

O

O

O

O

O

O

Propynyl-Dendron-Generation-4-hexadecihydroxide FORMULA: C

78H

124O

46







DDN1180.0500 500 mg € 480,00

DDN1180.1000 1 g € 840,00

O

O

O

O

O

O

O

O

OO

OO

OO

OO

OO O O

OO

O

O

O

O

O

O

O

O

OO O O

OO

O

O

O

O

O

O

O

O

O

O

Propynyl-Dendron-Generation-4-octaacetonide FORMULA: C

102H

156O

46



DDN1140.0500 500 mg € 700,00

DDN1140.1000 1 g € 1240,00

OH

OH

OHOH

OHOH

OH

OH

OH

OH

HOHO

OH

OH

HO

HO

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

OH

OH

OHOH

OHOH

OH

OH

OH

OH

HOHO

OH

OH

HO

HO

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

O

O

Propynyl-Dendron-Generation-5-dotriacontahydroxide FORMULA: C

158H

252O

94



DDN1190.0500 500 mg € 630,00

DDN1190.1000 1 g € 1110,00

O

O

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

O

O

Propynyl-Dendron-Generation-5-hexadeciacetonide FORMULA: C

206H

316O

94



4.2.3 Allyl DendronsDDN1200 Allyl-Dendron-G1-(OH)2 DDN1200.0500 500 mg € 230,00

DDN1200.1000 1 g € 370,00

DDN1200.5000 5 g € 1620,00OH

OH

O

O

Allyl-Dendron-Generation-1-dihydroxide, Allyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate FORMULA: C

8H

14O

4


DDN1250 Allyl-Dendron-G1-Acetonide DDN1250.0500 500 mg € 190,00

DDN1250.1000 1 g € 310,00

DDN1250.5000 5 g € 1300,00O

O

O

O

Allyl-Dendron-Generation-1-acetonide, allyl 2,2,5-trimethyl-1,3-dioxane-5-carboxylate FORMULA: C

11H

18O

4





DDN1210 Allyl-Dendron-G2-(OH)4 DDN1210.0500 500 mg € 300,00

DDN1210.1000 1 g € 510,00

DDN1210.5000 5 g € 2280,00

OH

OH

O

O

OH

OH

O

O

O

OAllyl-Dendron-Generation-2-tetrahydroxide, 2-(Allyloxycarbonyl)-2-methylpropane-1,3-diyl bis(3-hydroxy-2-(hydroxymethyl)-2-methylpro-panoate) FORMULA: C

18H

30O

10


DDN1260 Allyl-Dendron-G2-(Acetonide)2 DDN1260.0500 500 mg € 260,00

DDN1260.1000 1 g € 430,00

DDN1260.5000 5 g € 1900,00O

O

O

O

O

O

O

O

O

OAllyl-Dendron-Generation-2-diacetonide, 2-(Allyloxycarbonyl)-2-methyl-propane-1,3-diyl bis(2,2,5-trimethyl-1,3-dioxane-5-carboxylate) FORMULA: C

24H

38O

10



DDN1220.1000 1 g € 640,00

DDN1220.5000 5 g € 2880,00

HO HO

OO

OH

OH

O

O

O

O

HO HO

OO

OH

OH

O

O

O

O

O

O

Allyl-Dendron-Generation-3-octahydroxide FORMULA: C

38H

62O

22



DDN1270.1000 1 g € 570,00

DDN1270.5000 5 g € 2550,00

O

O

O

O

OO

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

Allyl-Dendron-Generation-3-tetraacetonide FORMULA: C

50H

78O

22



DDN1230.0500 500 mg € 560,00

DDN1230.1000 1 g € 980,00

OH

OH

OH

OH

OH

OH

OH

OH

OHOH

OHOH

HOHO

HOHO

OO O O

OO

O

O

O

O

O

O

O

O

OO O O

OO

O

O

O

O

O

O

O

O

O

O

Allyl-Dendron-Generation-4-hexadecihydroxide FORMULA: C

78H

126O

46



DDN1280.0500 500 mg € 480,00

DDN1280.1000 1 g € 840,00

O

O

O

O

O

O

O

O

OO

OO

OO

OO

OO O O

OO

O

O

O

O

O

O

O

O

OO O O

OO

O

O

O

O

O

O

O

O

O

O

Allyl-Dendron-Generation-4-octaacetonide FORMULA: C

102H

158O

46







DDN1240.0500 500 mg € 700,00

DDN1240.1000 1 g € 1240,00

OH

OH

OHOH

OHOH

OH

OH

OH

OH

HOHO

OH

OH

HO

HO

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

OH

OH

OHOH

OHOH

OH

OH

OH

OH

HOHO

OH

OH

HO

HO

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

O

O

Allyl-Dendron-Generation-5-dotriacontahydroxide FORMULA: C

158H

254O

94



DDN1290.0500 500 mg € 630,00

DDN1290.1000 1 g € 1110,00

O

O

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

O

O

Allyl-Dendron-Generation-5-hexadeciacetonide FORMULA: C

206H

318O

94


4.2.4 Disulfide bridged Dendrons DDN1300 SS-Dendrimer-G1-(OH)2 DDN1300.0250 250 mg € 230,00

DDN1300.1000 1 g € 590,00

DDN1300.5000 5 g € 2610,00OH

OHO

S SOO

HO

HOODithio-Bis(Dendrimer-Generation-1-dihydroxide),

2,2‘-Disulfanediylbis(ethane-2,1-diyl) bis(3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate) FORMULA: C

14H

26O

8S

2


DDN1350 SS-Dendrimer-G1-Acetonide DDN1350.0250 250 mg € 190,00

DDN1350.1000 1 g € 480,00

DDN1350.5000 5 g € 2120,00O

OO

S SOO

O

OODithio-Bis(Dendrimer-Generation-1-acetonide),

2,2‘-Disulfanediylbis(ethane-2,1-diyl) bis(2,2,5-trimethyl-1,3-dioxane-5-carboxylate) FORMULA: C

20H

34O

8S

2


DDN1310 SS-Dendrimer-G2-(OH)4 DDN1310.0250 250 mg € 300,00

DDN1310.1000 1 g € 820,00

DDN1310.5000 5 g € 3700,00OH

OH

OH

OH

O

O

O

O

O

S SOO

HO

HO

HO

HO

O

O

O

O

O

Dithio-Bis(Dendron-Generation-2-tetrahydroxide) FORMULA: C

34H

58O

20S

2


DDN1360 SS-Dendrimer-G2-(Acetonide)2 DDN1360.0250 250 mg € 260,00

DDN1360.1000 1 g € 700,00

DDN1360.5000 5 g € 3110,00O

O

O

O

O

O

O

O

O

S SOO

O

O

O

O

O

O

O

O

O

Dithio-Bis(Dendrimer-Generation-2-diacetonide), 2,2‘-(2,2‘-Disulfanediylbis(ethane-2,1-diyl)bis(oxy))bis(oxomethylene)bis(2-methylpropane-3,2,1-triyl) tetrakis(2,2,5-trimethyl-1,3-dioxane-5-carboxylate) FORMULA: C

46H

74O

20S

2







DDN1320.1000 1 g € 1040,00

DDN1320.5000 5 g € 4690,00

OH

OH

OH

OH

HOHO

HOHO

OO

O

O

O

O

OO

O

O

O

O

O

S SOO

HO

HO

HO

HO

OH OH

OH OH

OO

O

O

O

O

OO

O

O

O

O

O

Dithio-Bis(Dendrimer-Generation-3-octahydroxide) FORMULA: C

74H

122O

44S

2



DDN1370.1000 1 g € 930,00

DDN1370.5000 5 g € 4200,00

O

O

O

O

OO

OO

OO

O

O

O

O

OO

O

O

O

O

O

S SOO

O

O

O

O

O O

O O

OO

O

O

O

O

OO

O

O

O

O

O

Dithio-Bis(Dendrimer-Generation-3-tetraacetonide) FORMULA: C

98H

154O

44S

2



DDN1330.0250 250 mg € 560,00

DDN1330.1000 1 g € 1610,00

OH

OH

OH

OH

OH

OH

OH

OH

OHOH

OHOH

HOHO

HOHO

OO O O

OO

O

O

O

O

O

O

O

O

OO O O

OO

O

O

O

O

O

O

O

O

O

S SOO

HO

HO

HO

HO

HO

HO

HO

HO

HOHO

HOHO

OHOH

OHOH

O OOO

OO

O

O

O

O

O

O

O

O

O OOO

OO

O

O

O

O

O

O

O

O

O

Dithio-Bis(Dendrimer-Generation-4-hexadecihydroxide) FORMULA: C

154H

250O

92S

2



DDN1380.0250 250 mg € 480,00

DDN1380.1000 1 g € 1380,00

O

O

O

O

O

O

O

O

OO

OO

OO

OO

OO O O

OO

O

O

O

O

O

O

O

O

OO O O

OO

O

O

O

O

O

O

O

O

O

S SOO

O

O

O

O

O

O

O

O

OO

OO

OO

OO

O OOO

OO

O

O

O

O

O

O

O

O

O OOO

OO

O

O

O

O

O

O

O

O

O

Dithio-Bis(Dendrimer-Generation-4-octaacetonide) FORMULA: C

202H

314O

92S

2



DDN1340.0250 250 mg € 700,00

DDN1340.1000 1 g € 2030,00S S

OH

OH

OHOH

OHOH

OH

OH

OH

OH

HOHO

OH

OH

HO

HO

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

OH

OH

OHOH

OHOH

OH

OH

OH

OH

HOHO

OH

OH

HO

HO

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

O

O

HO

HO

HO HO

HOHO

HO

HO

HO

HO

OHOH

HO

HO

OH

OH

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

O O

OOO

O

OO

OO

O

HO

HO

HO HO

HOHO

HO

HO

HO

HO

OHOH

HO

HO

OH

OH

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

O O

OOO

O

OO

OO

O

O

O

O

O

Dithio-Bis(Dendrimer-Generation-5-dotriacontahydroxide) FORMULA: C

314H

506O

188S

2



DDN1390.0250 250 mg € 630,00

DDN1390.1000 1 g € 1820,00S S

O

O

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

OO

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

OO

O OO

O

OO

OO

O

O

O

O

O

O

O

O O

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

O O

OOO

O

OO

OO

O

O

O

O O

OO

O

O

O

O

OO

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

O

O

OO

O

O

O O

OOO

O

OO

OO

O

O

O

O

O

Dithio-Bis(Dendrimer-Generation-5-hexadeciacetonide) FORMULA: C

410H

634O

188S

2






4.2.5 PeG bridged DendronsDDN1400 Dendron-G1-PEG6-(OH)4 DDN1400.0250 250 mg € 250,00

DDN1400.0500 500 mg € 350,00

DDN1400.1000 1 g € 500,00

OH

OHO

OOHO

HOO

O

nTetra-hydroxy-alpha,omega-bis(Dendron-Generation-1) poly(ethylene glycol) (PEG-MW 6000 Da) MOLECULAR WEIGHT: 6000 Da

DDN1410 Dendron-G1-PEG20-(OH)4 DDN1410.0250 250 mg € 250,00

DDN1410.0500 500 mg € 325,00

DDN1410.1000 1 g € 475,00

OH

OHO

OOHO

HOO

O

nTetra-hydroxy-alpha,omega-bis(Dendron-Generation-1) poly(ethylene glycol) (PEG-MW 20000 Da) MOLECULAR WEIGHT: 20000 Da


DDN1420.0500 500 mg € 380,00

DDN1420.1000 1 g € 575,00OH

OH

OH

OH

O

O

O

O

O

OO

HO

HO

HO

HO

O

O

O

O

O

O

n

Octa-hydroxy-alpha,omega-bis(Dendron-Generation-2) poly(ethylene glycol) (PEG-MW 6000 Da) MOLECULAR WEIGHT: 6000 Da


DDN1430.0500 500 mg € 375,00

DDN1430.1000 1 g € 550,00OH

OH

OH

OH

O

O

O

O

O

OO

HO

HO

HO

HO

O

O

O

O

O

O

n

Octa-hydroxy-alpha,omega-bis(Dendron-Generation-2) poly(ethylene glycol) (PEG-MW 20000 Da) MOLECULAR WEIGHT: 20000 Da


DDN1440.0500 500 mg € 425,00

DDN1440.1000 1 g € 650,00

OH

OH

OH

OH

HOHO

HOHO

OO

O

O

O

O

OO

O

O

O

O

O

OOO

HO

HO

HO

HO

OH OH

OH OH

OO

O

O

O

O

OO

O

O

O

O

O

n

Hexadeci-hydroxy-alpha,omega-bis(Dendron-Generation-3) poly(ethylene glycol) (PEG-MW 6000 Da) MOLECULAR WEIGHT: 6000 Da


DDN1450.0500 500 mg € 400,00

DDN1450.1000 1 g € 600,00

OH

OH

OH

OH

HOHO

HOHO

OO

O

O

O

O

OO

O

O

O

O

O

OOO

HO

HO

HO

HO

OH OH

OH OH

OO

O

O

O

O

OO

O

O

O

O

O

n

Hexadeci-hydroxy-alpha,omega-bis(Dendron-Generation-3) poly(ethylene glycol) (PEG-MW 20000 Da) MOLECULAR WEIGHT: 20000 Da-




AAA1905 Aloc-O2Oc-OH*DCHA .........................................................................47BAA1466 Boc-O2Oc-OH*DCHA ......................................................................... 48BAA1485 Boc-O2Oc-O2Oc-OH .......................................................................... 48BAA5240 Boc-O1Pen-OH*DCHA ........................................................................ 48BAA6070 Boc,Pbf-amidino-O1Pen-OH ............................................................... 48BAA6080 Boc,Pbf-amidino-O2Oc-OH................................................................ 48BAL1047 Boc,Pbf-amidino-EEtOH .....................................................................81BAL1048 Boc,Pbf-amidino-EtOH .......................................................................81BNN1015 Boc-DODA ..........................................................................................77BNN1016 Boc-DOOA ..........................................................................................77BNN1017 Boc-EDA*HCl ......................................................................................77BNN1028 Boc-TOTA ............................................................................................78BNN1058 Boc-DSOA*HCl ....................................................................................77DAA1016 Dde-O2Oc-OH ..................................................................................... 51DDN1000 Azido-Dendron-G1-(OH)2 .................................................................. 150DDN1010 Azido-Dendron-G2-(OH)4 ................................................................. 150DDN1020 Azido-Dendron-G3-(OH)8 .................................................................. 151DDN1030 Azido-Dendron-G4-(OH)16 ................................................................. 151DDN1040 Azido-Dendron-G5-(OH)32 ................................................................ 151DDN1050 Azido-Dendron-G1-Acetonide............................................................ 150DDN1060 Azido-Dendron-G2-(Acetonide)2 ....................................................... 150DDN1070 Azido-Dendron-G3-(Acetonide)4 ....................................................... 151DDN1080 Azido-Dendron-G4-(Acetonide)8 ....................................................... 151DDN1090 Azido-Dendron-G5-(Acetonide)16 ...................................................... 151DDN1100 Alkynyl-Dendron-G1-(OH)2 ............................................................... 152DDN1110 Alkynyl-Dendron-G2-(OH)4 ............................................................... 152DDN1120 Alkynyl-Dendron-G3-(OH)8 .............................................................. 152DDN1130 Alkynyl-Dendron-G4-(OH)16 ............................................................. 152DDN1140 Alkynyl-Dendron-G5-(OH)32 ............................................................. 153DDN1150 Alkynyl-Dendron-G1-Acetonide ......................................................... 152DDN1160 Alkynyl-Dendron-G2-(Acetonide)2 .................................................... 152DDN1170 Alkynyl-Dendron-G3-(Acetonide)4 .................................................... 152DDN1180 Alkynyl-Dendron-G4-(Acetonide)8 .................................................... 153DDN1190 Alkynyl-Dendron-G5-(Acetonide)16 .................................................. 153DDN1200 Allyl-Dendron-G1-(OH)2 .................................................................... 153DDN1210 Allyl-Dendron-G2-(OH)4 ................................................................... 154DDN1220 Allyl-Dendron-G3-(OH)8 ................................................................... 154DDN1230 Allyl-Dendron-G4-(OH)16 .................................................................. 154DDN1240 Allyl-Dendron-G5-(OH)32 ................................................................. 155DDN1250 Allyl-Dendron-G1-Acetonide .............................................................. 153DDN1260 Allyl-Dendron-G2-(Acetonide)2 ......................................................... 154DDN1270 Allyl-Dendron-G3-(Acetonide)4 ........................................................ 154DDN1280 Allyl-Dendron-G4-(Acetonide)8 ........................................................ 154DDN1290 Allyl-Dendron-G5-(Acetonide)16 ....................................................... 155DDN1300 SS-Dendrimer-G1-(OH)2 .................................................................... 155DDN1310 SS-Dendrimer-G2-(OH)4 ................................................................... 155DDN1320 SS-Dendrimer-G3-(OH)8 ................................................................... 156DDN1330 SS-Dendrimer-G4-(OH)16 .................................................................. 156DDN1340 SS-Dendrimer-G5-(OH)32 ................................................................. 156DDN1350 SS-Dendrimer-G1-Acetonide ............................................................. 155DDN1360 SS-Dendrimer-G2-(Acetonide)2 ........................................................ 155DDN1370 SS-Dendrimer-G3-(Acetonide)4 ........................................................ 156DDN1380 SS-Dendrimer-G4-(Acetonide)8 ........................................................ 156DDN1390 SS-Dendrimer-G5-(Acetonide)16 ....................................................... 156DDN1400 Dendron-G1-PEG6-(OH)4 ...................................................................157DDN1410 Dendron-G1-PEG20-(OH)4 .................................................................157DDN1420 Dendron-G2-PEG6-(OH)8...................................................................157DDN1430 Dendron-G2-PEG20-(OH)8.................................................................157DDN1440 Dendron-G3-PEG6-(OH)16 .................................................................157DDN1450 Dendron-G3-PEG20-(OH)16 ...............................................................157DDN2000 PEG-Pentrimer-G1-(NH2+4xBoc-NH) ................................................. 148DDN2010 PEG-Pentrimer-G1-(Z-NH+4xBoc-NH) ................................................ 148DDN2020 PEG-Pentrimer-G1-(TFA-NH+4xBoc-NH) ............................................ 148DDN2030 PEG-Pentrimer-G1-(N3+4xBoc-NH).................................................... 148DDN2040 PEG-Pentrimer-G1-(N3+4xNH2)......................................................... 149DDN2050 PEG-Pentrimer-G1-(NH2+4xN3)......................................................... 149DDN2060 PEG-Pentrimer-G1-(Boc-NH+4xN3).................................................... 149FAA1435 Fmoc-O2Oc-OH ..................................................................................53FAA1565 Fmoc-O1Pen-OH .................................................................................53FAA1568 Fmoc-TTDS-OH ...................................................................................53FAA1787 Fmoc-O2Oc-O2Oc-OH ........................................................................53FAA6020 Fmoc-O2Oc-OPfp ................................................................................53FAA6580 Fmoc-O2Oc-NH-CH2-CH(OMe)2......................................................... 82

Indexcode Index

CODE NAME PAGE

CODE NAME PAGE

FAA6790 Fmoc-O2Oc-O2Oc-OPfp ......................................................................53FAL3010 Fmoc-O1Pen-ol .................................................................................. 82FNN1006 Fmoc-DODA*HCl ............................................................................... 79FNN1007 Fmoc-DOOA*HCl ............................................................................... 79FNN1008 Fmoc-EDA*HCl ................................................................................... 79FNN1011 Fmoc-TOTA*HCl ................................................................................. 79MAA1000 Mal-AMCHC-OSu................................................................................ 131MAA1010 Mmt-TTDS-OH ....................................................................................57MAA1020 Mal-beta-Ala-OSu .............................................................................. 131MAA5400 Mal-AMCHC-OH ................................................................................. 131PEG0173 H2N-[mPEG(4)]4................................................................................ 42PEG0183 NHS-[PEG(4)]4 ................................................................................... 44PEG0216 H2N-[mPEG(4)-mPEG(10)]2 ............................................................... 42PEG0306 Palm3-Cys-PEG-OH ............................................................................ 45PEG0506 Palm3-Cys-PEG-OH ............................................................................ 45PEG1000 H2N-PEG(20)-NH2 .............................................................................80PEG1001 H2N-PEG-NH2 ....................................................................................80PEG1002 H2N-PEG-NH2 ....................................................................................80PEG1003 H2N-PEG-NH2 ....................................................................................80PEG1004 H2N-PEG-NH2 ....................................................................................80PEG1005 H2N-PEG-NH2 ....................................................................................80PEG1006 H2N-PEG-OH ..................................................................................... 83PEG1007 H2N-PEG-OH ..................................................................................... 83PEG1008 H2N-PEG-OH ..................................................................................... 83PEG1009 HO-PEG(28)-OH ................................................................................ 143PEG1010 HO-PEG-OH ...................................................................................... 143PEG1011 HO-PEG-OH ...................................................................................... 143PEG1012 HO-PEG-OH ...................................................................................... 143PEG1013 HO-PEG-OH ...................................................................................... 143PEG1014 HO-PEG-OH ...................................................................................... 143PEG1015 HO-PEG(12)-OH ................................................................................. 143PEG1016 HO-PEG(8)-OH .................................................................................. 143PEG1017 HO-PEG-SH ....................................................................................... 129PEG1018 HO-PEG-SH ....................................................................................... 129PEG1019 HO-PEG-SH ....................................................................................... 129PEG1020 Boc-NH-PEG-OH .................................................................................81PEG1021 Boc-NH-PEG-OH .................................................................................81PEG1022 Boc-NH-PEG-OH .................................................................................81PEG1023 HO-PEG-STrt ..................................................................................... 129PEG1024 HO-PEG-STrt ..................................................................................... 129PEG1025 HO-PEG-STrt ..................................................................................... 129PEG1026 H2N-PEG-STrt.................................................................................... 124PEG1027 H2N-PEG-STrt.................................................................................... 124PEG1028 H2N-PEG-STrt.................................................................................... 124PEG1029 HO-PEG-CONH-NH-Boc .......................................................................81PEG1030 HO-PEG-CONH-NH-Boc .......................................................................81PEG1031 HO-PEG-CONH-NH-Boc .......................................................................81PEG1032 MeO-PEG(7)-OH ................................................................................ 144PEG1033 MeO-PEG-OH .................................................................................... 145PEG1034 MeO-PEG-OH .................................................................................... 145PEG1035 MeO-PEG-OH .................................................................................... 145PEG1036 MeO-PEG-OH .................................................................................... 145PEG1037 MeO-PEG-OH .................................................................................... 145PEG1038 MeO-PEG(11)-OH ............................................................................... 144PEG1044 Biotin-PEG(10)-NH2 .......................................................................... 103PEG1045 Biotin-PEG-NH2 ................................................................................ 103PEG1046 Biotin-PEG-NH2 ................................................................................ 103PEG1047 Biotin-PEG-NH2 ................................................................................ 103PEG1048 Biotin-PEG-mal ..................................................................................110PEG1049 Biotin-PEG-mal ..................................................................................110PEG1050 Biotin-PEG-mal ..................................................................................110PEG1051 Biotin-PEG(12)-COOH ........................................................................ 105PEG1052 Biotin-PEG-COOH ............................................................................. 105PEG1053 Biotin-PEG-COOH ............................................................................. 105PEG1054 Biotin-PEG-COOH ............................................................................. 105PEG1055 Biotin-PEG-NHS ................................................................................108PEG1056 Biotin-PEG-NHS ................................................................................108PEG1057 Biotin-PEG-NHS ................................................................................108PEG1058 mal-PEG-COOH ................................................................................. 134PEG1059 mal-PEG-COOH ................................................................................. 134PEG1060 mal-PEG-COOH ................................................................................. 134PEG1061 mal-PEG-NHS ................................................................................... 134PEG1062 mal-PEG-NHS ................................................................................... 134PEG1063 mal-PEG-NHS ................................................................................... 134PEG1065 Boc-NH-PEG(12)-NH2 ..........................................................................78PEG1066 Boc-NH-PEG(8)-NH2 ...........................................................................78PEG1067 Boc-NH-PEG-NH2 ................................................................................78PEG1068 Boc-NH-PEG-NH2 ................................................................................78



CODE NAME PAGE CODE NAME PAGE

PEG1069 Boc-NH-PEG-NH2 ................................................................................78PEG1070 Boc-NH-PEG(12)-COOH ...................................................................... 49PEG1071 Boc-NH-PEG(8)-COOH ....................................................................... 49PEG1072 Boc-NH-PEG-COOH ............................................................................ 50PEG1073 Boc-NH-PEG-COOH ............................................................................ 50PEG1074 Boc-NH-PEG-COOH ............................................................................ 50PEG1075 Br-PEG-Br .......................................................................................... 142PEG1076 Br-PEG-Br .......................................................................................... 142PEG1077 Br-PEG-Br .......................................................................................... 142PEG1078 Br-PEG-Br .......................................................................................... 142PEG1079 Br-PEG-Br .......................................................................................... 142PEG1080 Fmoc-NH-PEG(12)-COOH ................................................................... 54PEG1081 H2N-PEG(12)-N3 ................................................................................. 93PEG1082 HOOC-PEG-COOH ...............................................................................72PEG1083 HOOC-PEG-COOH ...............................................................................72PEG1084 HOOC-PEG-COOH ...............................................................................72PEG1085 HOOC-PEG-COOH ...............................................................................72PEG1086 HOOC-PEG-COOH ...............................................................................72PEG1087 H2N-PEG(7)-N3 .................................................................................. 93PEG1088 N3-PEG(8)-OH ................................................................................... 94PEG1090 HO-PEG(12)-CO-OtBu ......................................................................... 66PEG1091 HOOC-PEG(12)-COOH ......................................................................... 70PEG1092 HO-PEG-COOH ....................................................................................67PEG1093 HO-PEG-COOH ....................................................................................67PEG1094 HO-PEG-COOH ....................................................................................67PEG1095 H2N-PEG-COOH*HCl .......................................................................... 63PEG1096 H2N-PEG-COOH*HCl .......................................................................... 63PEG1097 H2N-PEG-COOH*HCl .......................................................................... 63PEG1098 HS-PEG-COOH .................................................................................. 120PEG1099 HS-PEG-COOH .................................................................................. 120PEG1100 HS-PEG-COOH .................................................................................. 120PEG1101 HS-PEG-CONH-NH-Boc ..................................................................... 125PEG1102 HS-PEG-CONH-NH-Boc ..................................................................... 125PEG1103 HS-PEG-CONH-NH-Boc ..................................................................... 125PEG1107 Fmoc-NH-PEG-COOH ......................................................................... 56PEG1108 Fmoc-NH-PEG-COOH ......................................................................... 56PEG1109 Fmoc-NH-PEG-COOH ......................................................................... 56PEG1110 Boc-NH-PEG-NHS ............................................................................... 50PEG1111 Boc-NH-PEG-NHS ............................................................................... 50PEG1112 Boc-NH-PEG-NHS ............................................................................... 50PEG1113 Boc-NH-PEG-SH ................................................................................ 124PEG1114 Boc-NH-PEG-SH ................................................................................ 124PEG1115 Boc-NH-PEG-SH ................................................................................ 124PEG1116 Fmoc-NH-PEG-NHS ............................................................................ 56PEG1117 Fmoc-NH-PEG-NHS ............................................................................ 56PEG1118 Fmoc-NH-PEG-NHS ............................................................................ 56PEG1119 HOOC-PEG(8)-SS-PEG(8)-COOH .........................................................119PEG1120 HS-PEG(8)-COOH ...............................................................................118PEG1121 HS-PEG-SH ........................................................................................ 130PEG1122 HS-PEG-SH ........................................................................................ 130PEG1123 HS-PEG-SH ........................................................................................ 130PEG1124 HS-PEG-SH ........................................................................................ 130PEG1125 HS-PEG-SH ........................................................................................ 130PEG1126 mal-PEG-mal .................................................................................... 139PEG1127 mal-PEG-mal .................................................................................... 139PEG1128 mal-PEG-mal .................................................................................... 139PEG1129 mal-PEG-mal .................................................................................... 139PEG1130 mal-PEG-mal .................................................................................... 139PEG1131 MeO-PEG-Br ..................................................................................... 142PEG1132 MeO-PEG-Br ..................................................................................... 142PEG1133 MeO-PEG-Br ..................................................................................... 142PEG1134 MeO-PEG-Br ..................................................................................... 142PEG1135 MeO-PEG-Br ..................................................................................... 142PEG1141 MeO-PEG-CHO ...................................................................................147PEG1142 MeO-PEG-CHO ...................................................................................147PEG1143 MeO-PEG-CHO ...................................................................................147PEG1144 MeO-PEG-CHO ...................................................................................147PEG1145 MeO-PEG-CHO ...................................................................................147PEG1146 MeO-PEG-mal ................................................................................... 138PEG1147 MeO-PEG-mal ................................................................................... 138PEG1148 MeO-PEG-mal ................................................................................... 138PEG1149 MeO-PEG-mal ................................................................................... 138PEG1150 MeO-PEG-mal ................................................................................... 138PEG1151 MeO-PEG-NH2 ................................................................................... 85PEG1152 MeO-PEG-NH2 ................................................................................... 85PEG1153 MeO-PEG-NH2 ................................................................................... 85PEG1154 MeO-PEG-NH2 ................................................................................... 85PEG1155 MeO-PEG-NH2 ................................................................................... 85

PEG1156 MeO-PEG(12)-COOH ............................................................................74PEG1157 MeO-PEG-COOH .................................................................................76PEG1158 MeO-PEG-COOH .................................................................................76PEG1159 MeO-PEG-COOH .................................................................................76PEG1160 MeO-PEG-COOH .................................................................................76PEG1161 MeO-PEG-COOH .................................................................................76PEG1162 MeO-PEG-NHS ....................................................................................76PEG1163 MeO-PEG-NHS ....................................................................................76PEG1164 MeO-PEG-NHS ....................................................................................76PEG1165 MeO-PEG-NHS ....................................................................................76PEG1166 MeO-PEG-NHS ....................................................................................76PEG1167 MeO-PEG(7)-SH................................................................................. 126PEG1168 MeO-PEG-SH ......................................................................................127PEG1169 MeO-PEG-SH ......................................................................................127PEG1170 MeO-PEG-SH ......................................................................................127PEG1171 MeO-PEG-SH ......................................................................................127PEG1172 MeO-PEG-SH ......................................................................................127PEG1178 OHC-PEG-CHO ...................................................................................147PEG1179 OHC-PEG-CHO ...................................................................................147PEG1180 OHC-PEG-CHO ...................................................................................147PEG1181 OHC-PEG-CHO ...................................................................................147PEG1182 OHC-PEG-CHO ...................................................................................147PEG1183 NHS-PEG-NHS.....................................................................................72PEG1184 NHS-PEG-NHS.....................................................................................72PEG1185 NHS-PEG-NHS.....................................................................................72PEG1186 NHS-PEG-NHS.....................................................................................72PEG1187 NHS-PEG-NHS.....................................................................................72PEG1188 NHS-PEG(8)-SS-PEG(8)-NHS ..............................................................119PEG1189 tBu-O2C-PEG(12)-COOH ...................................................................... 71PEG1195 MeO-PEG(7)-SS-PEG(7)-OMe ............................................................. 126PEG1196 H2N-PEG-SH*HCl .............................................................................. 124PEG1197 H2N-PEG-SH*HCl .............................................................................. 124PEG1198 H2N-PEG-SH*HCl .............................................................................. 124PEG1199 Trt-S-PEG-NHS .................................................................................. 120PEG1200 Trt-S-PEG-NHS .................................................................................. 120PEG1201 Trt-S-PEG-NHS .................................................................................. 120PEG1202 MeO-PEG-O-CO-NHS...........................................................................76PEG1203 Stea-O2Oc-OH ....................................................................................73PEG1204 H2N-PEG(8)-NH2 ...............................................................................80PEG1206 Biotin-PEG-OH ..................................................................................108PEG1207 Biotin-PEG-OH ..................................................................................108PEG1208 Epoxy-PEG-COOH .............................................................................. 66PEG1209 mal-PEG(27)-NHS ............................................................................. 134PEG1210 Fmoc-NH-PEG(27)-COOH ....................................................................55PEG1212 Biotin-PEG-SH ...................................................................................109PEG1213 Biotin-PEG-SH ...................................................................................109PEG1214 Biotin-PEG-SH ...................................................................................109PEG1215 OPSS-PEG-NHS ................................................................................. 123PEG1216 OPSS-PEG-NHS ................................................................................. 123PEG1217 OPSS-PEG-NHS ................................................................................. 123PEG1218 MeO-PEG-OMs .................................................................................. 145PEG1219 MeO-PEG-N3...................................................................................... 96PEG1220 N3-PEG(20)-OH.................................................................................. 94PEG1221 H-O2Oc-O2Oc-OH ............................................................................... 61PEG1222 ACRL-PEG-NHS ................................................................................... 65PEG1223 ACRL-PEG-NHS ................................................................................... 65PEG1224 ACRL-PEG-NHS ................................................................................... 65PEG1225 MeO-PEG-N3...................................................................................... 96PEG1226 Biotin-PEG-SH ...................................................................................109PEG1300 H2N-dPEG™(6)-COOH ........................................................................ 61PEG1305 H2N-dPEG™(6)-CO-OtBu ................................................................... 62PEG1310 H2N-dPEG™(12)-OH ........................................................................... 82PEG1315 H2N-dPEG™(12)-O-DMT .................................................................... 82PEG1320 H2N-dPEG™(4)-OH ............................................................................ 82PEG1325 H2N-dPEG™(4)-[mPEG(12)]3 ............................................................. 42PEG1335 H2N-dPEG™(4)-NHNH-Boc ................................................................ 79PEG1340 H2N-dPEG™(8)-OH............................................................................ 82PEG1345 H2N-dPEG™(12)-COOH ...................................................................... 62PEG1350 H2N-dPEG™(12)-CO-OtBu .................................................................. 62PEG1355 H2N-dPEG™(24)-COOH ..................................................................... 63PEG1360 H2N-dPEG™(24)-CO-OtBu ................................................................. 63PEG1365 H2N-EG2-CO-OtBu .............................................................................. 61PEG1370 H2N-dPEG™(4)-COOH ........................................................................ 61PEG1375 H2N-dPEG™(4)-CO-OtBu .................................................................... 61PEG1380 H2N-dPEG™(8)-COOH ....................................................................... 62PEG1385 H2N-dPEG™(8)-CO-OtBu ................................................................... 62PEG1390 N3-dPEG™(12)-OH ............................................................................. 94PEG1395 N3-dPEG™(12)-NHS ............................................................................97



CODE NAME PAGE

PEG1400 N3-dPEG™(4)-NHS ............................................................................ 96PEG1405 N3-dPEG™(8)-NHS .............................................................................97PEG1415 Biotin-dPEG™(3)-Benzophenone .......................................................101PEG1420 Biotin-dPEG™(3)-Cyanocobalamin ................................................... 102PEG1425 Biotin-dPEG™(4)-NHNH2 ................................................................. 102PEG1430 HOOC-PEG(4)-COOH .......................................................................... 69PEG1435 NHS-dPEG™(4)-NHS .......................................................................... 69PEG1450 HOOC-dPEG™(6)-COOH .................................................................... 69PEG1460 NHS-dPEG™(8)-NHS .......................................................................... 70PEG1465 HOOC-dPEG™(28)-COOH ................................................................... 71PEG1475 HOOC-dPEG™(8)-COOH .................................................................... 70PEG1480 Bis-mal-Oc-NH2*TFA ......................................................................... 45PEG1485 mal-dPEG™(3)-mal ........................................................................... 139PEG1490 HOOC-PEG(4)-[mPEG(12)]3 ................................................................ 43PEG1495 Z-NH-dPEG™(4)-COOH ...................................................................... 64PEG1500 H2N-dPEG™(11)-NH2 .........................................................................80PEG1515 Biotin-dPEG™(4)-COOH.................................................................... 105PEG1525 Fmoc-NH-(dPEG™(4)-Biotin)-COOH .................................................106PEG1535 HO-dPEG™(4)-CO-OtBu ..................................................................... 66PEG1540 HO-dPEG™(8)-CO-OtBu ..................................................................... 66PEG1545 Rhodamine B-dPEG™(4)-COOH .........................................................77PEG1550 mal-dPEG™(12)-NHS .........................................................................133PEG1555 mal-EG(2)-COOH .............................................................................. 132PEG1560 mal-EG(2)-NHS ................................................................................. 132PEG1565 mal-dPEG™(24)-NHS ........................................................................ 134PEG1570 mal-dPEG™(4)-COOH ....................................................................... 132PEG1575 mal-dPEG™(4)-NHS .......................................................................... 132PEG1580 mal-dPEG™(4)-NHNH-Boc ................................................................ 136PEG1585 mal-dPEG™(6)-NHS ..........................................................................133PEG1590 mal-dPEG™(8)-NHS ..........................................................................133PEG1595 Biotin-dPEG™(11)-mal ........................................................................110PEG1600 mal-dPEG™(24)-COOH ..................................................................... 134PEG1605 Biotin-dPEG™(3)-mal ........................................................................110PEG1610 mal-PEG(4)-[mPEG(12)]3.................................................................... 45PEG1615 mal-dPEG™(8)-COOH ........................................................................133PEG1620 MeO-dPEG™(3)-COOH .......................................................................73PEG1625 MeO-dPEG™(8)-COOH .......................................................................74PEG1630 MeO-EPr-COOH ..................................................................................73PEG1635 MeO-dPEG™(24)-COOH ......................................................................75PEG1645 MeO-dPEG™(11)-O-CO-NHS ................................................................74PEG1655 MeO-dPEG™(12)-NH2 ........................................................................ 84PEG1660 MeO-dPEG™(12)-N3 ........................................................................... 95PEG1665 MeO-dPEG™(12)-mal .........................................................................137PEG1670 MeO-dPEG™(24)-NH2 ....................................................................... 84PEG1675 MeO-dPEG™(24)-mal ........................................................................137PEG1680 MeO-dPEG™(3)-O-CO-NHS .................................................................74PEG1685 MeO-dPEG™(4)-NH2 ......................................................................... 84PEG1690 MeO-dPEG™(4)-N3 ............................................................................ 95PEG1695 MeO-dPEG™(4)-Tos .......................................................................... 144PEG1700 MeO-dPEG™(8)-NH2 ......................................................................... 84PEG1705 MeO-dPEG™(8)-N3 ............................................................................ 95PEG1710 MeO-dPEG™(24)-N3 .......................................................................... 95PEG1720 MeO-EG(2)-Tos .................................................................................. 144PEG1730 MeO-PEG(7)-NH2 ............................................................................... 84PEG1735 Mmt-S-dPEG™(8)-COOH ...................................................................118PEG1740 Mmt-S-dPEG™(4)-COOH ....................................................................118PEG1745 Z-NH-dPEG™(3)-NH2 .........................................................................80PEG1785 Z-NH-dPEG™(12)-COOH ..................................................................... 64PEG1790 Z-NH-dPEG™(24)-COOH .................................................................... 65PEG1795 Z-NH-dPEG™(6)-COOH ...................................................................... 64PEG1800 Z-NH-dPEG™(8)-COOH ...................................................................... 64PEG1805 Fmoc-NH-dPEG™(4)-NHNH-Boc ........................................................ 79PEG1810 Fmoc-AEEP .........................................................................................53PEG1815 Fmoc-NH-dPEG™(24)-COOH ..............................................................55PEG1820 Fmoc-NH-dPEG™(4)-COOH ............................................................... 54PEG1825 Fmoc-NH-dPEG™(6)-COOH ............................................................... 54PEG1830 Fmoc-NH-dPEG™(8)-COOH ............................................................... 54PEG1840 NHS-dPEG™(4)-[mPEG(12)]3 ............................................................. 44PEG1845 Biotin-dPEG™(4)-NHS-(Biotinidase resistant) ..................................106PEG1855 NHS-dPEG™(4)-NHNH-Boc ................................................................ 49PEG1860 Biotin-dPEG™(12)-NHS .....................................................................108PEG1870 Biotin-dPEG™(4)-NHS ......................................................................106PEG1880 MeO-dPEG™(3)-NHS ..........................................................................73PEG1885 MeO-dPEG™(8)-NHS ..........................................................................74PEG1890 MeO-dPEG™(12)-NHS .........................................................................74PEG1895 MeO-dPEG™(16)-NHS .........................................................................75PEG1900 MeO-dPEG™(24)-NHS ........................................................................75PEG1905 MeO-EPr-NHS .....................................................................................73

PEG1910 Biotin-dPEG™(4)-S-S-NHS ................................................................ 107PEG1915 Boc-NH-dPEG™(4)-OH ........................................................................81PEG1920 Boc-NH-dPEG™(4)-COOH .................................................................. 48PEG1925 Bzl-O-dPEG™(4)-COOH...................................................................... 66PEG1935 Propargyl-NHS ....................................................................................87PEG1940 Ac-S-dPEG™(4)-COOH ....................................................................... 117PEG1945 Ac-S-dPEG™(4)-NHS .......................................................................... 117PEG1950 Ac-S-dPEG™(8)-COOH ....................................................................... 117PEG1955 Ac-S-dPEG™(8)-NHS .......................................................................... 117PEG1960 Boc-NH-dPEG™(12)-OH .......................................................................81PEG1970 HS-dPEG™(4)-COOH..........................................................................118PEG1980 Trt-S-dPEG™(4)-COOH .......................................................................118PEG1985 DIG(Pfp)2 ........................................................................................... 68PEG1990 DIG(NHS)2 ......................................................................................... 68PEG2000 HS-FA-PEG(12)-COOH .........................................................................119PEG2005 HS-FA-PEG(28)-COOH ........................................................................119PEG2010 HS-FA-PEG(8)-OH .............................................................................. 128PEG2015 N3-PEG(9)-COOH ................................................................................97PEG2020 DOHA .................................................................................................73PEG2025 TODA ..................................................................................................73PEG2030 TUDA ................................................................................................. 68PEG2035 DOODA .............................................................................................. 68PEG2040 MeO-PEG-N3...................................................................................... 96PEG2045 MeO-PEG-N3...................................................................................... 96PEG2050 MeO-PEG-N3...................................................................................... 96PEG2060 6-arm-mPEG-NHS .............................................................................. 44PEG2065 Biotin-TEG-ATFBA .............................................................................. 99PEG2065 Biotin-TEG-ATFBA ..............................................................................101PEG2070 Biotin-TEG-OPfp ................................................................................106PEG2080 Biotin-TEG-Biotin ................................................................................111PEG2085 mal-PEG(12)-mal ............................................................................... 139PEG2090 MBS ................................................................................................... 131PEG2095 Ac-S-TEG-OH ..................................................................................... 128PEG2105 MP-EDA*TFA ..................................................................................... 136PEG2110 Biotin-TEG-NH2*TFA ......................................................................... 103PEG2115 NHS-PEG(4)-CO-OBzl ......................................................................... 69PEG2125 mal-PEG(12)-COOH ............................................................................133PEG2135 mal-COOH ......................................................................................... 131PEG2140 Biotin-PEG(3+4)-N3 ........................................................................... 98PEG2140 Biotin-PEG(3+4)-N3 ...........................................................................101PEG2145 Dnp-NH-PEG(4)-COOH ........................................................................52PEG2150 Dnp-NH-PEG(4)-NHS ..........................................................................52PEG2155 MeO-PEG(4)-OH ............................................................................... 144PEG2160 Mmt-NH-PEG(4)-COOH .......................................................................57PEG2166 Biotin-PEG(4)-Lys(PEG(4)-Biotin)-PEG(4)-TFP ....................................101PEG2170 MeO-PEG(4)-CHO ............................................................................. 146PEG2175 MeO-PEG(8)-CHO ............................................................................. 146PEG2180 MeO-PEG(24)-CHO ............................................................................ 146PEG2185 MBz-PEG(4)-COOH ............................................................................ 135PEG2190 MBz-PEG(4)-NHS .............................................................................. 135PEG2195 MBz-PEG(8)-COOH ........................................................................... 135PEG2200 MBz-PEG(8)-NHS .............................................................................. 135PEG2205 MBz-PEG(12)-COOH........................................................................... 135PEG2210 MBz-PEG(12)-NHS ............................................................................. 135PEG2215 MBz-PEG(24)-COOH .......................................................................... 135PEG2220 MBz-PEG(24)-NHS ............................................................................. 135PEG2225 OPSS-PEG(4)-COOH .......................................................................... 122PEG2230 OPSS-PEG(4)-NHS ............................................................................. 122PEG2235 OPSS-PEG(8)-COOH .......................................................................... 122PEG2240 OPSS-PEG(8)-NHS ............................................................................ 122PEG2245 OPSS-PEG(12)-COOH ......................................................................... 122PEG2250 OPSS-PEG(12)-NHS............................................................................ 122PEG2255 OPSS-PEG(24)-COOH ........................................................................ 123PEG2260 OPSS-PEG(24)-NHS ........................................................................... 123PEG2265 Mmt-NH-PEG(8)-COOH .......................................................................57PEG2270 Mmt-NH-PEG(12)-COOH ..................................................................... 58PEG2275 Mmt-NH-PEG(16)-COOH ..................................................................... 58PEG2280 Mmt-NH-PEG(24)-COOH .................................................................... 59PEG2285 Dnp-NH-PEG(12)-COOH ......................................................................52PEG2290 Dnp-NH-PEG(12)-NHS .........................................................................52PEG2295 H2N-mPEG(4)-[mPEG(4)]3 ................................................................. 42PEG2300 NHS-PEG(4)-[mPEG(4)]3 .................................................................... 44PEG2305 HOOC-PEG(4)-[mPEG(4)]3 ................................................................. 43PEG2310 mal-PEG(4)-[mPEG(4)]3 ..................................................................... 44PEG2315 H2N-PEG(4)-[mPEG(8)]3 .................................................................... 42PEG2320 NHS-PEG(4)-[mPEG(8)]3 .................................................................... 44PEG2325 HOOC-PEG(4)-[mPEG(8)]3 ................................................................. 43PEG2335 MeO-PEG(11)-PrCHO .......................................................................... 146

CODE NAME PAGE



PEG2340 mal-PEG(4)-[mPEG(8)]3 .................................................................... 45PEG2345 N3-PEG(4)-COOH ............................................................................... 96PEG2350 H2N-PEG(8)-N3 .................................................................................. 93PEG2355 HO-PEG(6)-CO-OtBu .......................................................................... 66PEG2365 HO-PEG(24)-CO-tBu ............................................................................67PEG2370 MeO-PEG(16)-COOH ...........................................................................74PEG2375 MeO-PEG(4)-mal ...............................................................................137PEG2380 MeO-PEG(8)-mal ...............................................................................137PEG2385 Mmt-NH-PEG(4)-CO-OPfp ...................................................................57PEG2390 Mmt-NH-PEG(8)-CO-OPfp .................................................................. 58PEG2395 Mmt-NH-PEG(12)-CO-OPfp ................................................................. 58PEG2400 Mmt-NH-PEG(16)-CO-OPfp ................................................................. 58PEG2405 Mmt-NH-PEG(24)-CO-OPfp ................................................................ 59PEG2410 Boc-NH-PEG(8)-COOH ....................................................................... 49PEG2415 Boc-NH-PEG(12)-COOH ...................................................................... 49PEG2420 H-O2Oc-OH......................................................................................... 61PEG2430 H-O2Oc-OtBu*HCI .............................................................................. 61PEG2470 Ac-S-OEG-OH .................................................................................... 128PEG2550 Biotin-Sar-OH ................................................................................... 104PEG2555 Biotin-2-Abu-OH ............................................................................... 104PEG2560 Biotinyl-O2Oc-OH ............................................................................. 105PEG2565 Biotinyl-O2Oc-O2Oc-OH ................................................................... 105PEG2755 Propargyl amine .................................................................................87PEG2760 Biotin-DOOA*HCl.............................................................................. 102PEG2770 H-O2Oc-O2Oc-O2Oc-OH ..................................................................... 61PEG2780 N3-O2Oc-OH*CHA ............................................................................. 96PEG2790 N3-O2Oc-O2Oc-OH*CHA ....................................................................97PEG2800 MeO-PEG-alkyne ................................................................................87PEG2810 MeO-PEG-alkyne ................................................................................87PEG2820 MeO-PEG-alkyne ................................................................................87PEG2830 MeO-PEG-alkyne ................................................................................87PEG2840 MeO-PEG-alkyne ................................................................................87PEG2850 NHS-PEG-alkyne ................................................................................ 89PEG2860 NHS-PEG-alkyne ................................................................................ 89PEG2870 NHS-PEG-alkyne ................................................................................ 89PEG2880 NHS-PEG-alkyne ................................................................................ 89PEG2900 NHS-PEG(NH-Boc)-alkyne .................................................................. 90PEG2910 NHS-PEG(NH-Boc)-alkyne .................................................................. 90PEG2920 NHS-PEG(NH-Boc)-alkyne .................................................................. 90PEG2930 NHS-PEG(NH-Boc)-alkyne .................................................................. 90PEG2950 H2N-PEG-alkyne ................................................................................ 88PEG2960 H2N-PEG-alkyne ................................................................................ 88PEG2970 H2N-PEG-alkyne ................................................................................ 88PEG2980 H2N-PEG-alkyne ................................................................................ 88PEG3000 H2N-PEG-N3 ...................................................................................... 94PEG3010 H2N-PEG-N3 ...................................................................................... 94PEG3020 H2N-PEG-N3 ...................................................................................... 94PEG3030 H2N-PEG-N3 ...................................................................................... 94PEG3040 H2N-PEG(11)-N3 ................................................................................. 93PEG3050 H2N-PEG(9)-N3 .................................................................................. 93PEG3060 H2N-PEG(3)-N3 .................................................................................. 93PEG3070 H2N-PEG(23)-N3 ................................................................................ 93PEG3080 H2N-PEG(35)-N3 ................................................................................ 93PEG3090 I-PEG-alkyne ...................................................................................... 88PEG3100 I-PEG-alkyne ...................................................................................... 88PEG3110 I-PEG-alkyne ...................................................................................... 88PEG3120 I-PEG-alkyne ...................................................................................... 88PEG3130 I-PEG-N3 ............................................................................................ 98PEG3140 I-PEG-N3 ............................................................................................ 98PEG3150 I-PEG-N3 ............................................................................................ 98PEG3160 I-PEG-N3 ............................................................................................ 98PEG3170 HOOC-PEG(3)-COOH .......................................................................... 69PEG3180 Fmoc-NH-PEG(16)-COOH ....................................................................55PEG3190 MeO-dPEG™(37)-NHS .........................................................................75PEG3200 MeO-dPEG™(49)-NHS ........................................................................75PEG3210 MeO-dPEG™(37)-COOH ......................................................................75PEG3220 MeO-dPEG™(49)-COOH .....................................................................75PEG3230 NHS-PEG(4)-[mPEG(24)]3 .................................................................. 44PEG3240 HOOC-PEG(4)-[mPEG(24)]3 ............................................................... 43PEG3250 MeO-dPEG™(15)-OH ......................................................................... 145PEG3260 MeO-dPEG™(19)-OH ......................................................................... 145PEG3270 MeO-dPEG™(23)-OH ........................................................................ 145PEG3280 MeO-dPEG™(36)-OH ........................................................................ 145PEG3290 MeO-dPEG™(15)-NH2 ........................................................................ 84PEG3300 MeO-dPEG™(36)-NH2 ....................................................................... 84PEG3310 MeO-dPEG™(48)-NH2 ....................................................................... 84PEG3320 H2N-dPEG™(16)-COOH ...................................................................... 62PEG3330 H2N-dPEG™(20)-COOH ..................................................................... 62

PEG3340 H2N-dPEG™(36)-COOH ..................................................................... 63PEG3350 H2N-PEG(4)-[mdPEG™(24)]3 ............................................................. 42PEG3360 MeO-dPEG™(36)-mal ........................................................................137PEG3370 MeO-dPEG™(48)-mal ........................................................................137PEG3380 MeO-dPEG™(7)-O-CO-NHS .................................................................74PEG3390 MeO-dPEG™(15)-O-CO-NHS ................................................................74PEG3400 MeO-dPEG™(19)-O-CO-NHS ...............................................................75PEG3410 MeO-dPEG™(23)-O-CO-NHS ...............................................................75PEG3420 mal-PEG(4)-[mPEG(24)]3 ................................................................... 45PEG3430 MeO-dPEG™(36)-N3 .......................................................................... 95PEG3440 HS-dPEG™(12)-COOH ........................................................................118PEG3450 HS-dPEG™(16)-COOH ........................................................................119PEG3460 HS-dPEG™(20)-COOH .......................................................................119PEG3470 MeO-dPEG™(4)-SH ........................................................................... 126PEG3480 MeO-dPEG™(8)-SH ........................................................................... 126PEG3490 MeO-dPEG™(12)-SH .......................................................................... 126PEG3500 Lipoamide-dPEG™(4)-COOH ............................................................. 113PEG3510 Lipoamide-dPEG™(8)-COOH ............................................................. 113PEG3520 Lipoamide-dPEG™(12)-COOH ............................................................ 113PEG3530 Lipoamide-dPEG™(16)-COOH ............................................................ 113PEG3540 Lipoamide-dPEG™(20)-COOH ........................................................... 113PEG3550 Lipoamide-dPEG™(3)-mal ................................................................. 114PEG3560 Lipoamide-dPEG™(11)-mal ................................................................ 114PEG3570 Lipoamide-dPEG™(3)-biotin ............................................................. 113PEG3580 Lipoamide-dPEG™(11)-biotin ............................................................. 113PEG3590 Lipoamide-dPEG™(4)-OMe ............................................................... 114PEG3600 Lipoamide-dPEG™(8)-OMe ............................................................... 114PEG3610 Lipoamide-dPEG™(12)-OMe .............................................................. 114PEG3620 Lipoamide-dPEG™(24)-OMe ............................................................. 114PEG3630 Ac-S-dPEG™(12)-NHS ......................................................................... 117PEG3640 Ac-S-dPEG™(16)-NHS ......................................................................... 117PEG3650 Ac-S-dPEG™(20)-NHS ........................................................................ 117PEG3660 Ac-S-dPEG™(12)-COOH ...................................................................... 117PEG3670 Ac-S-dPEG™(16)-COOH ...................................................................... 117PEG3680 Ac-S-dPEG™(20)-COOH ..................................................................... 117PEG3690 H2N-dPEG™(16)-CO-OtBu .................................................................. 62PEG3700 H2N-dPEG™(20)-CO-OtBu ................................................................. 63PEG3710 H2N-dPEG™(36)-CO-OtBu ................................................................. 63PEG3720 HO-dPEG™(16)-COOH.........................................................................67PEG3730 HO-dPEG™(20)-COOH ........................................................................67PEG3740 H2N-dPEG™(24)-OH .......................................................................... 82PEG3750 H2N-dPEG™(36)-OH .......................................................................... 82PEG3760 N3-dPEG™(4)-OH .............................................................................. 94PEG3770 N3-dPEG™(24)-OH ............................................................................ 95PEG3780 N3-dPEG™(36)-OH ............................................................................ 95PEG3790 Ac-S-dPEG™(12)-OH .......................................................................... 128PEG3800 Ac-S-dPEG™(16)-OH.......................................................................... 128PEG3810 Ac-S-dPEG™(20)-OH ......................................................................... 128PEG3820 MeO-dPEG™(7)-Tos........................................................................... 144PEG3830 mal-dPEG™(16)-NHS .........................................................................133PEG3840 mal-dPEG™(20)-NHS.........................................................................133PEG3850 mal-dPEG™(6)-COOH ....................................................................... 132PEG3860 mal-dPEG™(16)-COOH.......................................................................133PEG3870 mal-dPEG™(20)-COOH ......................................................................133PEG3880 mal-dPEG™(8)-NHNH-Boc ............................................................... 136PEG3890 mal-dPEG™(12)-NHNH-Boc .............................................................. 136PEG3900 OPSS-dPEG™(16)-NHS ...................................................................... 122PEG3910 OPSS-dPEG™(20)-NHS ..................................................................... 123PEG3920 OPSS-dPEG™(36)-NHS ..................................................................... 123PEG3930 OPSS-dPEG™(16)-COOH ................................................................... 122PEG3940 OPSS-dPEG™(20)-COOH .................................................................. 122PEG3950 OPSS-dPEG™(36)-COOH .................................................................. 123PEG3960 NHS-dPEG™(4)-NHS .......................................................................... 69PEG3970 NHS-dPEG™(6)-NHS .......................................................................... 69PEG3980 NHS-dPEG™(12)-NHS ......................................................................... 70PEG3990 NHS-dPEG™(16)-NHS ........................................................................ 70PEG4000 NHS-dPEG™(20)-NHS ......................................................................... 71PEG4010 NHS-dPEG™(24)-NHS ......................................................................... 71PEG4020 Pfp-DOODA-Pfp ................................................................................. 68PEG4030 Pfp-TUDA-Pfp ..................................................................................... 68PEG4040 Pfp-dPEG™(3)-Pfp .............................................................................. 69PEG4050 Pfp-dPEG™(4)-Pfp.............................................................................. 69PEG4060 Pfp-dPEG™(6)-Pfp ............................................................................. 70PEG4070 Pfp-dPEG™(8)-Pfp ............................................................................. 70PEG4080 Pfp-dPEG™(12)-Pfp ............................................................................ 70PEG4090 Pfp-dPEG™(16)-Pfp ............................................................................. 71PEG4100 Pfp-dPEG™(20)-Pfp ............................................................................ 71PEG4110 Tfp-dPEG™(24)-Tfp ............................................................................. 71




PEG4120 NHS-DOODA-NHS .............................................................................. 68PEG4130 NHS-TUDA-NHS ................................................................................. 68PEG4140 HOOC-dPEG™(16)-COOH ................................................................... 70PEG4150 HOOC-dPEG™(20)-COOH ................................................................... 71PEG4160 HOOC-dPEG™(24)-COOH.................................................................... 71PEG4170 N3-dPEG™(8)-COOH ..........................................................................97PEG4180 N3-dPEG™(12)-COOH .........................................................................97PEG4190 N3-dPEG™(24)-COOH .........................................................................97PEG4230 H2N-dPEG™(8)-NHNH-Boc ................................................................ 79PEG4240 H2N-dPEG™(12)-NHNH-Boc ............................................................... 79PEG4250 Biotin-dPEG™(24)-NHS .....................................................................108PEG4260 Biotin-dPEG™(24)-COOH .................................................................. 105PEG4270 Biotin-dPEG™(48)-COOH ................................................................. 105PEG4290 Biotin-dPEG™(7)-NH2 ....................................................................... 103PEG4300 Biotin-dPEG™(11)-NH2 ...................................................................... 103PEG4310 Biotin-dPEG™(23)-NH2 ..................................................................... 103PEG4320 Biotin-dPEG™(23)-mal ......................................................................110PEG4330 Biotin-dPEG™(7)-N3 .......................................................................... 99PEG4330 Biotin-dPEG™(7)-N3 ......................................................................... 104PEG4340 Biotin-dPEG™(11)-N3 ......................................................................... 99PEG4340 Biotin-dPEG™(11)-N3 ........................................................................ 104PEG4350 Biotin-dPEG™(23)-N3 ........................................................................ 99PEG4350 Biotin-dPEG™(23)-N3 ....................................................................... 104PEG4360 Biotin-dPEG™(47)-N3 ........................................................................ 99PEG4360 Biotin-dPEG™(47)-N3 ....................................................................... 104PEG4370 Fmoc-NH-dPEG™(3)-COOH ................................................................53PEG4380 Fmoc-NH-dPEG™(5)-COOH ............................................................... 54PEG4390 Fmoc-NH-dPEG™(20)-COOH ..............................................................55PEG4400 Fmoc-NH-dPEG™(36)-COOH ..............................................................55PEG4410 Fmoc-NH-dPEG™(4)-NHS .................................................................. 54PEG4420 Fmoc-NH-dPEG™(8)-NHS .................................................................. 54PEG4430 Fmoc-NH-dPEG™(12)-NHS ................................................................. 54PEG4440 Fmoc-L-Lys(dPEG™(4)-Biotin)-OH......................................................101PEG4450 Fmoc-L-Lys(dPEG™(12)-Biotin)-OH ....................................................101PEG4460 Boc-NH-dPEG™(16)-COOH ................................................................. 49PEG4470 Boc-NH-dPEG™(20)-COOH ................................................................ 49PEG4480 Boc-NH-dPEG™(24)-COOH ................................................................ 49PEG4490 Boc-NH-dPEG™(36)-COOH ................................................................ 50PEG4500 Mmt-NH-dPEG™(4)-TFP......................................................................57PEG4510 Mmt-NH-dPEG™(8)-TFP .................................................................... 58PEG4520 Mmt-NH-dPEG™(12)-TFP ................................................................... 58PEG4530 Mmt-NH-dPEG™(16)-TFP ................................................................... 58PEG4540 Mmt-NH-dPEG™(20)-TFP .................................................................. 59PEG4550 Mmt-NH-dPEG™(24)-TFP ................................................................... 59PEG4560 Mmt-NH-dPEG™(36)-TFP ................................................................... 59PEG4570 Z-NH-dPEG™(16)-COOH ..................................................................... 64PEG4580 Z-NH-dPEG™(20)-COOH .................................................................... 64PEG4590 Z-NH-dPEG™(36)-COOH .................................................................... 65PEG4600 Mmt-S-dPEG™(12)-COOH...................................................................119PEG4610 Mmt-S-dPEG™(16)-COOH ..................................................................119PEG4620 Mmt-S-dPEG™(20)-COOH..................................................................119PEG4630 Phth-NO-dPEG™(12)-NHS ...................................................................55PEG4640 Aminoxy-dPEG™(12+12)-[mdPEG™(11)]3 ........................................... 43PEG4650 Mtt-O2Oc-OH*DEA .............................................................................57PEG4660 Amino-dPEG™(11)-aminoxy-Boc .........................................................78PEG4670 Fmoc-NH-O-dPEG™(12)-COOH ...........................................................55PEG4680 Biotin-dPEG™(11)-O-NH2*HCl ........................................................... 103PEG4690 FB-dPEG™(12)-TFP ............................................................................. 65PEG4700 FB-dPEG™(24)-TFP ............................................................................ 65PEG4705 Biotin-PEG(11)-SH ..............................................................................108PEG4710 Z-O1Pen-OH ....................................................................................... 64PEG4715 OPSS-PEG-OPSS ............................................................................... 130PEG4720 OPSS-PEG-NHS ................................................................................. 123PEG4725 OPSS-PEG-OPSS ............................................................................... 130PEG4730 OPSS-PEG-OPSS ............................................................................... 130PEG4735 OPSS-PEG-OPSS ............................................................................... 130PEG4740 OPSS-PEG-OPSS ............................................................................... 130PEG4745 MeO-PEG-OPSS .................................................................................127PEG4750 MeO-PEG-OPSS .................................................................................127PEG4755 MeO-PEG-OPSS .................................................................................127PEG4760 MeO-PEG-OPSS .................................................................................127PEG4765 MeO-PEG-OPSS .................................................................................127PEG4770 Biotin-PEG-OPSS...............................................................................109PEG4775 Biotin-PEG-OPSS...............................................................................109PEG4780 Biotin-PEG-OPSS...............................................................................109PEG4785 Biotin-PEG-OPSS...............................................................................109PEG4790 MeO-PEG-Si(OMe)3 .......................................................................... 140PEG4795 MeO-PEG-Si(OMe)3 .......................................................................... 140

PEG4800 MeO-PEG-Si(OMe)3 .......................................................................... 140PEG4805 MeO-PEG-Si(OMe)3 .......................................................................... 140PEG4810 Alkyne-PEG-Si(OMe)3 .........................................................................91PEG4810 Alkyne-PEG-Si(OMe)3 ....................................................................... 140PEG4815 Alkyne-PEG-Si(OMe)3 .........................................................................91PEG4815 Alkyne-PEG-Si(OMe)3 ....................................................................... 140PEG4820 Alkyne-PEG-Si(OMe)3 .........................................................................91PEG4820 Alkyne-PEG-Si(OMe)3 ........................................................................ 141PEG4825 Alkyne-PEG-Si(OMe)3 .........................................................................91PEG4825 Alkyne-PEG-Si(OMe)3 ........................................................................ 141PEG4830 Azido-PEG-Si(OMe)3 .........................................................................100PEG4830 Azido-PEG-Si(OMe)3 .......................................................................... 141PEG4835 Azido-PEG-Si(OMe)3 .........................................................................100PEG4835 Azido-PEG-Si(OMe)3 .......................................................................... 141PEG4840 Azido-PEG-Si(OMe)3 .........................................................................100PEG4840 Azido-PEG-Si(OMe)3 .......................................................................... 141PEG4845 Azido-PEG-Si(OMe)3 .........................................................................100PEG4845 Azido-PEG-Si(OMe)3 .......................................................................... 141PEG4850 Biotin-PEG-Si(OMe)3 ..........................................................................111PEG4850 Biotin-PEG-Si(OMe)3 ......................................................................... 141PEG4855 Biotin-PEG-Si(OMe)3 ..........................................................................111PEG4855 Biotin-PEG-Si(OMe)3 ......................................................................... 141PEG4860 Biotin-PEG-Si(OMe)3 ..........................................................................111PEG4860 Biotin-PEG-Si(OMe)3 ......................................................................... 141PEG4865 Biotin-PEG-Si(OMe)3 ..........................................................................111PEG4865 Biotin-PEG-Si(OMe)3 ......................................................................... 141PGA1000 nBu-PGA(10)[Na] ................................................................................24PGA1005 nBu-PGA(20)[Na]................................................................................24PGA1010 nBu-PGA(50)[Na]................................................................................24PGA1015 nBu-PGA(100)[Na] ..............................................................................24PGA1020 nBu-PGA(200)[Na] .............................................................................24PGA1025 nBu-PGA(300)[Na] .............................................................................24PGA1030 nBu-PGA(400)[Na] .............................................................................24PGA1035 nBu-PGA(800)[Na] .............................................................................24PGA1040 Npt-PGA(10)[Na] ................................................................................ 25PGA1045 Npt-PGA(20)[Na] ............................................................................... 25PGA1050 Npt-PGA(50)[Na] ............................................................................... 25PGA1055 Npt-PGA(100)[Na] .............................................................................. 25PGA1060 Npt-PGA(200)[Na] ............................................................................. 25PGA1065 Npt-PGA(300)[Na] ............................................................................. 25PGA1070 Npt-PGA(400)[Na] ............................................................................. 25PGA1075 Npt-PGA(800)[Na] ............................................................................. 25PGA1080 Prg-PGA(10)[Na] ................................................................................. 26PGA1085 Prg-PGA(20)[Na] ................................................................................ 26PGA1090 Prg-PGA(50)[Na] ................................................................................ 26PGA1095 Prg-PGA(100)[Na]............................................................................... 26PGA1100 Prg-PGA(200)[Na] .............................................................................. 26PGA1105 Prg-PGA(300)[Na] .............................................................................. 26PGA1110 Prg-PGA(400)[Na] .............................................................................. 26PGA1115 Prg-PGA(800)[Na] .............................................................................. 26PGA1120 N3-PGA(10)[Na] ..................................................................................27PGA1125 N3-PGA(20)[Na] .................................................................................27PGA1130 N3-PGA(50)[Na] .................................................................................27PGA1135 N3-PGA(100)[Na] ................................................................................27PGA1140 N3-PGA(200)[Na] ...............................................................................27PGA1145 N3-PGA(300)[Na] ...............................................................................27PGA1150 N3-PGA(400)[Na] ...............................................................................27PGA1155 N3-PGA(800)[Na] ...............................................................................27PGA1160 nBu-PGA(10)[Prg(10)] ......................................................................... 28PGA1165 nBu-PGA(20)[Prg(10)] ........................................................................ 28PGA1170 nBu-PGA(50)[Prg(10)] ........................................................................ 28PGA1175 nBu-PGA(100)[Prg(10)] ....................................................................... 28PGA1175 nBu-PGA(100)[Prg(10)] ....................................................................... 30PGA1180 nBu-PGA(200)[Prg(10)] ...................................................................... 28PGA1180 nBu-PGA(200)[Prg(10)] ....................................................................... 31PGA1185 nBu-PGA(10)[Prg(20)] ........................................................................ 28PGA1185 nBu-PGA(10)[Prg(20)] ......................................................................... 31PGA1190 nBu-PGA(20)[Prg(20)] ........................................................................ 28PGA1190 nBu-PGA(20)[Prg(20)] ......................................................................... 31PGA1195 nBu-PGA(50)[Prg(20)] ........................................................................ 29PGA1195 nBu-PGA(50)[Prg(20)] ......................................................................... 31PGA1200 nBu-PGA(100)[Prg(20)] ...................................................................... 29PGA1200 nBu-PGA(100)[Prg(20)] ....................................................................... 31PGA1205 nBu-PGA(200)[Prg(20)]...................................................................... 29PGA1205 nBu-PGA(200)[Prg(20)]....................................................................... 31PGA1210 Npt-PGA(10)[Prg(10)] .......................................................................... 29PGA1210 Npt-PGA(10)[Prg(10)] ........................................................................... 31PGA1215 Npt-PGA(20)[Prg(10)] ......................................................................... 29




PGA1215 Npt-PGA(20)[Prg(10)] .......................................................................... 31PGA1220 Npt-PGA(50)[Prg(10)] ......................................................................... 29PGA1220 Npt-PGA(50)[Prg(10)] ..........................................................................32PGA1225 Npt-PGA(100)[Prg(10)] ....................................................................... 29PGA1225 Npt-PGA(100)[Prg(10)] ........................................................................32PGA1230 Npt-PGA(200)[Prg(10)] ....................................................................... 29PGA1230 Npt-PGA(200)[Prg(10)] ........................................................................32PGA1235 Npt-PGA(10)[Prg(20)] ......................................................................... 30PGA1235 Npt-PGA(10)[Prg(20)] ..........................................................................32PGA1240 Npt-PGA(20)[Prg(20)] ........................................................................ 30PGA1240 Npt-PGA(20)[Prg(20)] .........................................................................32PGA1245 Npt-PGA(50)[Prg(20)] ........................................................................ 30PGA1245 Npt-PGA(50)[Prg(20)] .........................................................................32PGA1250 Npt-PGA(100)[Prg(20)] ....................................................................... 30PGA1250 Npt-PGA(100)[Prg(20)] ........................................................................32PGA1255 Npt-PGA(200)[Prg(20)] ...................................................................... 30PGA1255 Npt-PGA(200)[Prg(20)] .......................................................................32PGA1260 nBu-PGA(10)[PEG2-N3(10)] ................................................................ 30PGA1260 nBu-PGA(10)[PEG2-N3(10)] .................................................................32PGA1265 nBu-PGA(20)[PEG2-N3(10)]................................................................ 30PGA1265 nBu-PGA(20)[PEG2-N3(10)].................................................................32PGA1270 nBu-PGA(50)[PEG2-N3(10)]................................................................ 30PGA1270 nBu-PGA(50)[PEG2-N3(10)].................................................................33PGA1275 nBu-PGA(100)[PEG2-N3(10)] ...............................................................33PGA1280 nBu-PGA(200)[PEG2-N3(10)] ..............................................................33PGA1285 nBu-PGA(10)[PEG2-N3(20)].................................................................33PGA1290 nBu-PGA(20)[PEG2-N3(20)] ................................................................33PGA1295 nBu-PGA(50)[PEG2-N3(20)] ................................................................33PGA1300 nBu-PGA(100)[PEG2-N3(20)] ..............................................................33PGA1305 nBu-PGA(200)[PEG2-N3(20)] ..............................................................33PGA1310 Npt-PGA(10)[PEG2-N3(10)] ................................................................. 34PGA1315 Npt-PGA(20)[PEG2-N3(10)] ................................................................ 34PGA1320 Npt-PGA(50)[PEG2-N3(10)] ................................................................ 34PGA1325 Npt-PGA(100)[PEG2-N3(10)] ............................................................... 34PGA1330 Npt-PGA(200)[PEG2-N3(10)] .............................................................. 34PGA1335 Npt-PGA(10)[PEG2-N3(20)] ................................................................ 34PGA1340 Npt-PGA(20)[PEG2-N3(20)] ............................................................... 34PGA1345 Npt-PGA(50)[PEG2-N3(20)] ............................................................... 34PGA1350 Npt-PGA(100)[PEG2-N3(20)] .............................................................. 34PGA1355 Npt-PGA(200)[PEG2-N3(20)] ............................................................. 34PGA1360 nBu-PGA(10)[PEG7-N3(10)] .................................................................35PGA1365 nBu-PGA(20)[PEG7-N3(10)] .................................................................35PGA1370 nBu-PGA(50)[PEG7-N3(10)] .................................................................35PGA1375 nBu-PGA(100)[PEG7-N3(10)] ...............................................................35PGA1380 nBu-PGA(200)[PEG7-N3(10)] ...............................................................35PGA1385 nBu-PGA(10)[PEG7-N3(20)] .................................................................35PGA1390 nBu-PGA(20)[PEG7-N3(20)] ................................................................35PGA1395 nBu-PGA(50)[PEG7-N3(20)] ................................................................35PGA1400 nBu-PGA(100)[PEG7-N3(20)] ...............................................................35PGA1405 nBu-PGA(200)[PEG7-N3(20)] ..............................................................35PGA1410 Npt-PGA(10)[PEG7-N3(10)] ................................................................. 36PGA1415 Npt-PGA(20)[PEG7-N3(10)] ................................................................ 36PGA1420 Npt-PGA(50)[PEG7-N3(10)] ................................................................ 36PGA1425 Npt-PGA(100)[PEG7-N3(10)] ............................................................... 36PGA1430 Npt-PGA(200)[PEG7-N3(10)] .............................................................. 36PGA1435 Npt-PGA(10)[PEG7-N3(20)] ................................................................ 36PGA1440 Npt-PGA(20)[PEG7-N3(20)] ................................................................ 36PGA1445 Npt-PGA(50)[PEG7-N3(20)] ................................................................ 36PGA1450 Npt-PGA(100)[PEG7-N3(20)] .............................................................. 36PGA1455 Npt-PGA(200)[PEG7-N3(20)].............................................................. 36PGA1460 nBu-PGA(10)[mPEG(10)] .....................................................................37PGA1465 nBu-PGA(20)[mPEG(10)] .....................................................................37PGA1470 nBu-PGA(50)[mPEG(10)] .....................................................................37PGA1475 nBu-PGA(100)[mPEG(10)] ...................................................................37PGA1480 nBu-PGA(200)[mPEG(10)] ..................................................................37PGA1485 nBu-PGA(10)[mPEG(20)] .....................................................................37PGA1490 nBu-PGA(20)[mPEG(20)] ....................................................................37PGA1495 nBu-PGA(50)[mPEG(20)] ....................................................................37PGA1500 nBu-PGA(100)[mPEG(20)] ................................................................. 38PGA1505 nBu-PGA(200)[mPEG(20)] ................................................................. 38PGA1510 Npt-PGA(10)[mPEG(10)] ..................................................................... 38PGA1515 Npt-PGA(20)[mPEG(10)] .................................................................... 38PGA1520 Npt-PGA(50)[mPEG(10)] .................................................................... 38PGA1525 Npt-PGA(100)[mPEG(10)] ................................................................... 38PGA1530 Npt-PGA(200)[mPEG(10)] .................................................................. 38PGA1535 Npt-PGA(10)[mPEG(20)] .................................................................... 38PGA1540 Npt-PGA(20)[mPEG(20)] .................................................................... 38PGA1545 Npt-PGA(50)[mPEG(20)] .................................................................... 38

PGA1550 Npt-PGA(100)[mPEG(20)] .................................................................. 39PGA1555 Npt-PGA(200)[mPEG(20)] ................................................................. 39PGA1560 Prg-PGA(10)[mPEG(10)] ...................................................................... 39PGA1565 Prg-PGA(20)[mPEG(10)] ..................................................................... 39PGA1570 Prg-PGA(50)[mPEG(10)] ..................................................................... 39PGA1575 Prg-PGA(100)[mPEG(10)] .................................................................... 39PGA1580 Prg-PGA(200)[mPEG(10)] ................................................................... 39PGA1585 Prg-PGA(10)[mPEG(20)] ..................................................................... 40PGA1590 Prg-PGA(20)[mPEG(20)] .................................................................... 40PGA1595 Prg-PGA(50)[mPEG(20)] .................................................................... 40PGA1600 Prg-PGA(100)[mPEG(20)] ................................................................... 40PGA1605 Prg-PGA(200)[mPEG(20)] .................................................................. 40PGA1610 N3-PGA(10)[mPEG(10)] ....................................................................... 41PGA1615 N3-PGA(20)[mPEG(10)] ....................................................................... 41PGA1620 N3-PGA(50)[mPEG(10)]....................................................................... 41PGA1625 N3-PGA(100)[mPEG(10)] ..................................................................... 41PGA1630 N3-PGA(200)[mPEG(10)] .................................................................... 41PGA1635 N3-PGA(10)[mPEG(20)] ....................................................................... 41PGA1640 N3-PGA(20)[mPEG(20)] ...................................................................... 41PGA1645 N3-PGA(50)[mPEG(20)] ...................................................................... 41PGA1650 N3-PGA(100)[mPEG(20)] .................................................................... 41PGA1655 N3-PGA(200)[mPEG(20)] .................................................................... 41RL-1020 DTT (racemic) .................................................................................... 115ZAA1186 Z-O2Oc-OH*DCHA ............................................................................. 64




6-arm-mPEG-NHS .......................................................................... PEG2060 ......... 44Ac-S-dPEG™(12)-COOH................................................................... PEG3660 ......... 117Ac-S-dPEG™(12)-NHS ..................................................................... PEG3630 .......... 117Ac-S-dPEG™(12)-OH ....................................................................... PEG3790 ......... 128Ac-S-dPEG™(16)-COOH .................................................................. PEG3670 .......... 117Ac-S-dPEG™(16)-NHS ..................................................................... PEG3640 ......... 117Ac-S-dPEG™(16)-OH ....................................................................... PEG3800 ........ 128Ac-S-dPEG™(20)-COOH.................................................................. PEG3680 ......... 117Ac-S-dPEG™(20)-NHS .................................................................... PEG3650 .......... 117Ac-S-dPEG™(20)-OH ...................................................................... PEG3810 ......... 128Ac-S-dPEG™(4)-COOH .................................................................... PEG1940 .......... 117Ac-S-dPEG™(4)-NHS ...................................................................... PEG1945 .......... 117Ac-S-dPEG™(8)-COOH ................................................................... PEG1950 .......... 117Ac-S-dPEG™(8)-NHS ...................................................................... PEG1955........... 117Ac-S-OEG-OH ................................................................................. PEG2470 ......... 128Ac-S-TEG-OH .................................................................................. PEG2095......... 128ACRL-PEG-NHS ............................................................................... PEG1222 ........... 65ACRL-PEG-NHS ............................................................................... PEG1223 ........... 65ACRL-PEG-NHS ............................................................................... PEG1224 ........... 65Alkyne-PEG-Si(OMe)3 .................................................................... PEG4810 ...........91Alkyne-PEG-Si(OMe)3 .................................................................... PEG4810 ......... 140Alkyne-PEG-Si(OMe)3 .................................................................... PEG4815 ...........91Alkyne-PEG-Si(OMe)3 .................................................................... PEG4815 ......... 140Alkyne-PEG-Si(OMe)3 .................................................................... PEG4820 ..........91Alkyne-PEG-Si(OMe)3 .................................................................... PEG4820 ......... 141Alkyne-PEG-Si(OMe)3 .................................................................... PEG4825 ...........91Alkyne-PEG-Si(OMe)3 .................................................................... PEG4825 .......... 141Alkynyl-Dendron-G1-(OH)2 ............................................................. DDN1100 ......... 152Alkynyl-Dendron-G1-Acetonide ...................................................... DDN1150 ......... 152Alkynyl-Dendron-G2-(Acetonide)2 ................................................. DDN1160 ......... 152Alkynyl-Dendron-G2-(OH)4 ............................................................ DDN1110.......... 152Alkynyl-Dendron-G3-(Acetonide)4 ................................................. DDN1170 ......... 152Alkynyl-Dendron-G3-(OH)8 ............................................................ DDN1120 ......... 152Alkynyl-Dendron-G4-(Acetonide)8 ................................................. DDN1180 ......... 153Alkynyl-Dendron-G4-(OH)16 ........................................................... DDN1130 ......... 152Alkynyl-Dendron-G5-(Acetonide)16 ................................................ DDN1190 ......... 153Alkynyl-Dendron-G5-(OH)32 .......................................................... DDN1140 ......... 153Allyl-Dendron-G1-(OH)2 ................................................................. DDN1200 ........ 153Allyl-Dendron-G1-Acetonide ........................................................... DDN1250 ........ 153Allyl-Dendron-G2-(Acetonide)2 ...................................................... DDN1260 ........ 154Allyl-Dendron-G2-(OH)4 ................................................................. DDN1210 ......... 154Allyl-Dendron-G3-(Acetonide)4 ...................................................... DDN1270 ......... 154Allyl-Dendron-G3-(OH)8 ................................................................ DDN1220 ........ 154Allyl-Dendron-G4-(Acetonide)8 ...................................................... DDN1280 ........ 154Allyl-Dendron-G4-(OH)16 ............................................................... DDN1230 ........ 154Allyl-Dendron-G5-(Acetonide)16..................................................... DDN1290 ........ 155Allyl-Dendron-G5-(OH)32 ............................................................... DDN1240 ........ 155Aloc-O2Oc-OH*DCHA ..................................................................... AAA1905 ...........47Amino-dPEG™(11)-aminoxy-Boc..................................................... PEG4660 ..........78Aminoxy-dPEG™(12+12)-[mdPEG™(11)]3 ........................................ PEG4640 ......... 43Azido-Dendron-G1-(OH)2 ............................................................... DDN1000 ........ 150Azido-Dendron-G1-Acetonide ......................................................... DDN1050 ........ 150Azido-Dendron-G2-(Acetonide)2 .................................................... DDN1060 ........ 150Azido-Dendron-G2-(OH)4 ............................................................... DDN1010 ......... 150Azido-Dendron-G3-(Acetonide)4 .................................................... DDN1070 ......... 151Azido-Dendron-G3-(OH)8 .............................................................. DDN1020 ......... 151Azido-Dendron-G4-(Acetonide)8 .................................................... DDN1080 ......... 151Azido-Dendron-G4-(OH)16 ............................................................. DDN1030 ......... 151Azido-Dendron-G5-(Acetonide)16................................................... DDN1090 ......... 151Azido-Dendron-G5-(OH)32 ............................................................. DDN1040 ......... 151Azido-PEG-Si(OMe)3 ...................................................................... PEG4830 ........100Azido-PEG-Si(OMe)3 ...................................................................... PEG4830 ......... 141Azido-PEG-Si(OMe)3 ...................................................................... PEG4835 .........100Azido-PEG-Si(OMe)3 ...................................................................... PEG4835 .......... 141Azido-PEG-Si(OMe)3 ...................................................................... PEG4840 ........100Azido-PEG-Si(OMe)3 ...................................................................... PEG4840 ......... 141Azido-PEG-Si(OMe)3 ...................................................................... PEG4845 .........100Azido-PEG-Si(OMe)3 ...................................................................... PEG4845 .......... 141Biotin-2-Abu-OH ............................................................................. PEG2555 ......... 104Biotin-DOOA*HCl ........................................................................... PEG2760 ......... 102Biotin-dPEG™(11)-mal .................................................................... PEG1595...........110Biotin-dPEG™(11)-N3 ...................................................................... PEG4340 .......... 99Biotin-dPEG™(11)-N3 ...................................................................... PEG4340 ......... 104Biotin-dPEG™(11)-NH2 ................................................................... PEG4300 ........ 103Biotin-dPEG™(11)-O-NH2*HCl ........................................................ PEG4680 ........ 103Biotin-dPEG™(12)-NHS ................................................................... PEG1860 .........108

Name Index NAME CODE PAGE

NAME CODE PAGE Biotin-dPEG™(23)-mal ................................................................... PEG4320 ..........110Biotin-dPEG™(23)-N3 ..................................................................... PEG4350 .......... 99Biotin-dPEG™(23)-N3 ..................................................................... PEG4350 ......... 104Biotin-dPEG™(23)-NH2 .................................................................. PEG4310 ......... 103Biotin-dPEG™(24)-COOH ............................................................... PEG4260 ........ 105Biotin-dPEG™(24)-NHS .................................................................. PEG4250 .........108Biotin-dPEG™(3)-Benzophenone ................................................... PEG1415 ...........101Biotin-dPEG™(3)-Cyanocobalamin ................................................ PEG1420 ......... 102Biotin-dPEG™(3)-mal ..................................................................... PEG1605 ..........110Biotin-dPEG™(4)-COOH ................................................................. PEG1515 .......... 105Biotin-dPEG™(4)-NHNH2 ............................................................... PEG1425 .......... 102Biotin-dPEG™(4)-NHS .................................................................... PEG1870 ..........106Biotin-dPEG™(4)-NHS-(Biotinidase resistant)................................ PEG1845 .........106Biotin-dPEG™(4)-S-S-NHS .............................................................. PEG1910 .......... 107Biotin-dPEG™(47)-N3 ..................................................................... PEG4360.......... 99Biotin-dPEG™(47)-N3 ..................................................................... PEG4360......... 104Biotin-dPEG™(48)-COOH ............................................................... PEG4270 ......... 105Biotin-dPEG™(7)-N3 ....................................................................... PEG4330 .......... 99Biotin-dPEG™(7)-N3 ....................................................................... PEG4330 ......... 104Biotin-dPEG™(7)-NH2 .................................................................... PEG4290 ........ 103Biotin-PEG-COOH ........................................................................... PEG1052 ......... 105Biotin-PEG-COOH ........................................................................... PEG1053 ......... 105Biotin-PEG-COOH ........................................................................... PEG1054 ......... 105Biotin-PEG-mal .............................................................................. PEG1048 ..........110Biotin-PEG-mal .............................................................................. PEG1049 ..........110Biotin-PEG-mal .............................................................................. PEG1050 ..........110Biotin-PEG-NH2 .............................................................................. PEG1045 ......... 103Biotin-PEG-NH2 .............................................................................. PEG1046 ......... 103Biotin-PEG-NH2 .............................................................................. PEG1047 .......... 103Biotin-PEG-NHS.............................................................................. PEG1055 .........108Biotin-PEG-NHS.............................................................................. PEG1056 .........108Biotin-PEG-NHS.............................................................................. PEG1057 ..........108Biotin-PEG-OH ............................................................................... PEG1206 .........108Biotin-PEG-OH ............................................................................... PEG1207 ..........108Biotin-PEG-OPSS ............................................................................ PEG4770 .........109Biotin-PEG-OPSS ............................................................................ PEG4775 .........109Biotin-PEG-OPSS ............................................................................ PEG4780 .........109Biotin-PEG-OPSS ............................................................................ PEG4785 .........109Biotin-PEG-SH ................................................................................ PEG1212 ..........109Biotin-PEG-SH ................................................................................ PEG1213...........109Biotin-PEG-SH ................................................................................ PEG1214 ..........109Biotin-PEG-SH ................................................................................ PEG1226 ..........109Biotin-PEG-Si(OMe)3 ...................................................................... PEG4850 ..........111Biotin-PEG-Si(OMe)3 ...................................................................... PEG4850 ......... 141Biotin-PEG-Si(OMe)3 ...................................................................... PEG4855 ...........111Biotin-PEG-Si(OMe)3 ...................................................................... PEG4855 .......... 141Biotin-PEG-Si(OMe)3 ...................................................................... PEG4860 ..........111Biotin-PEG-Si(OMe)3 ...................................................................... PEG4860 ......... 141Biotin-PEG-Si(OMe)3 ...................................................................... PEG4865...........111Biotin-PEG-Si(OMe)3 ...................................................................... PEG4865.......... 141Biotin-PEG(10)-NH2 ........................................................................ PEG1044 ......... 103Biotin-PEG(11)-SH ........................................................................... PEG4705 .........108Biotin-PEG(12)-COOH ..................................................................... PEG1051 .......... 105Biotin-PEG(3+4)-N3 ........................................................................ PEG2140 .......... 98Biotin-PEG(3+4)-N3 ........................................................................ PEG2140 ..........101Biotin-PEG(4)-Lys(PEG(4)-Biotin)-PEG(4)-TFP ................................. PEG2166 ..........101Biotin-Sar-OH ................................................................................. PEG2550 ......... 104Biotin-TEG-ATFBA ........................................................................... PEG2065.......... 99Biotin-TEG-ATFBA ........................................................................... PEG2065..........101Biotin-TEG-Biotin ........................................................................... PEG2080 ..........111Biotin-TEG-NH2*TFA ...................................................................... PEG2110 .......... 103Biotin-TEG-OPfp ............................................................................. PEG2070 .........106Biotinyl-O2Oc-O2Oc-OH ................................................................ PEG2565 ......... 105Biotinyl-O2Oc-OH .......................................................................... PEG2560......... 105Bis-mal-Oc-NH2*TFA ...................................................................... PEG1480 .......... 45Boc-DODA ...................................................................................... BNN1015 ...........77Boc-DOOA ...................................................................................... BNN1016 ...........77Boc-DSOA*HCl ............................................................................... BNN1058 ..........77Boc-EDA*HCl .................................................................................. BNN1017............77Boc-NH-dPEG™(4)-COOH .............................................................. PEG1920 .......... 48Boc-NH-dPEG™(12)-OH .................................................................. PEG1960 ...........81Boc-NH-dPEG™(16)-COOH ............................................................. PEG4460 ......... 49Boc-NH-dPEG™(20)-COOH ............................................................ PEG4470 .......... 49Boc-NH-dPEG™(24)-COOH ............................................................. PEG4480 ......... 49Boc-NH-dPEG™(36)-COOH ............................................................ PEG4490 ......... 50Boc-NH-dPEG™(4)-OH ................................................................... PEG1915 ............81Boc-NH-PEG-COOH ........................................................................ PEG1072 ........... 50Boc-NH-PEG-COOH ........................................................................ PEG1073 ........... 50



NAME CODE PAGE NAME CODE PAGE

Boc-NH-PEG-COOH ........................................................................ PEG1074 ........... 50Boc-NH-PEG-NH2 ........................................................................... PEG1067............78Boc-NH-PEG-NH2 ........................................................................... PEG1068 ...........78Boc-NH-PEG-NH2 ........................................................................... PEG1069 ...........78Boc-NH-PEG-NHS ........................................................................... PEG1110 ............ 50Boc-NH-PEG-NHS ........................................................................... PEG1111 ............. 50Boc-NH-PEG-NHS ........................................................................... PEG1112 ............ 50Boc-NH-PEG-OH ............................................................................. PEG1020 ...........81Boc-NH-PEG-OH ............................................................................. PEG1021 ............81Boc-NH-PEG-OH ............................................................................. PEG1022 ...........81Boc-NH-PEG-SH .............................................................................. PEG1113 ........... 124Boc-NH-PEG-SH .............................................................................. PEG1114 ........... 124Boc-NH-PEG-SH .............................................................................. PEG1115 ........... 124Boc-NH-PEG(12)-COOH ................................................................... PEG1070 .......... 49Boc-NH-PEG(12)-COOH ................................................................... PEG2415 ........... 49Boc-NH-PEG(12)-NH2 ...................................................................... PEG1065 ...........78Boc-NH-PEG(8)-COOH .................................................................... PEG1071 ........... 49Boc-NH-PEG(8)-COOH .................................................................... PEG2410 .......... 49Boc-NH-PEG(8)-NH2....................................................................... PEG1066 ...........78Boc-O1Pen-OH*DCHA ..................................................................... BAA5240 .......... 48Boc-O2Oc-O2Oc-OH ....................................................................... BAA1485 .......... 48Boc-O2Oc-OH*DCHA ...................................................................... BAA1466 .......... 48Boc-TOTA ........................................................................................ BNN1028 ..........78Boc,Pbf-amidino-EEtOH ................................................................. BAL1047 ............81Boc,Pbf-amidino-EtOH ................................................................... BAL1048............81Boc,Pbf-amidino-O1Pen-OH ........................................................... BAA6070 .......... 48Boc,Pbf-amidino-O2Oc-OH ............................................................ BAA6080 ......... 48Br-PEG-Br ....................................................................................... PEG1075 .......... 142Br-PEG-Br ....................................................................................... PEG1076.......... 142Br-PEG-Br ....................................................................................... PEG1077 .......... 142Br-PEG-Br ....................................................................................... PEG1078.......... 142Br-PEG-Br ....................................................................................... PEG1079.......... 142Bzl-O-dPEG™(4)-COOH .................................................................. PEG1925 ........... 66Dde-O2Oc-OH ................................................................................ DAA1016............ 51Dendron-G1-PEG20-(OH)4 .............................................................. DDN1410 ..........157Dendron-G1-PEG6-(OH)4 ................................................................ DDN1400 .........157Dendron-G2-PEG20-(OH)8 ............................................................. DDN1430 .........157Dendron-G2-PEG6-(OH)8 ............................................................... DDN1420 .........157Dendron-G3-PEG20-(OH)16 ............................................................ DDN1450 .........157Dendron-G3-PEG6-(OH)16 .............................................................. DDN1440 .........157DIG(NHS)2 ..................................................................................... PEG1990 .......... 68DIG(Pfp)2 ....................................................................................... PEG1985 .......... 68Dnp-NH-PEG(12)-COOH .................................................................. PEG2285 ...........52Dnp-NH-PEG(12)-NHS ..................................................................... PEG2290 ...........52Dnp-NH-PEG(4)-COOH ................................................................... PEG2145 ............52Dnp-NH-PEG(4)-NHS ...................................................................... PEG2150 ...........52DOHA ............................................................................................. PEG2020 ..........73DOODA .......................................................................................... PEG2035 .......... 68DTT (racemic) ................................................................................ RL-1020 ............ 115Epoxy-PEG-COOH........................................................................... PEG1208 .......... 66FB-dPEG™(12)-TFP ......................................................................... PEG4690 ......... 65FB-dPEG™(24)-TFP ......................................................................... PEG4700 .......... 65Fmoc-AEEP ..................................................................................... PEG1810 ............53Fmoc-DODA*HCl ............................................................................ FNN1006 ......... 79Fmoc-DOOA*HCl ............................................................................ FNN1007 .......... 79Fmoc-EDA*HCl ............................................................................... FNN1008 ......... 79Fmoc-L-Lys(dPEG™(12)-Biotin)-OH ................................................. PEG4450..........101Fmoc-L-Lys(dPEG™(4)-Biotin)-OH .................................................. PEG4440 .........101Fmoc-NH-(dPEG™(4)-Biotin)-COOH ............................................... PEG1525 ..........106Fmoc-NH-dPEG™(24)-COOH .......................................................... PEG1815 ............55Fmoc-NH-dPEG™(4)-COOH ............................................................ PEG1820 .......... 54Fmoc-NH-dPEG™(6)-COOH ........................................................... PEG1825........... 54Fmoc-NH-dPEG™(8)-COOH ........................................................... PEG1830 .......... 54Fmoc-NH-dPEG™(12)-NHS ............................................................. PEG4430 .......... 54Fmoc-NH-dPEG™(20)-COOH.......................................................... PEG4390...........55Fmoc-NH-dPEG™(3)-COOH ............................................................ PEG4370 ...........53Fmoc-NH-dPEG™(36)-COOH .......................................................... PEG4400 ..........55Fmoc-NH-dPEG™(4)-NHNH-Boc .................................................... PEG1805 .......... 79Fmoc-NH-dPEG™(4)-NHS .............................................................. PEG4410 .......... 54Fmoc-NH-dPEG™(5)-COOH ............................................................ PEG4380 ......... 54Fmoc-NH-dPEG™(8)-NHS .............................................................. PEG4420 ......... 54Fmoc-NH-O-dPEG™(12)-COOH ....................................................... PEG4670 ...........55Fmoc-NH-PEG-COOH ..................................................................... PEG1107 ........... 56Fmoc-NH-PEG-COOH ..................................................................... PEG1108 ........... 56Fmoc-NH-PEG-COOH ..................................................................... PEG1109 ........... 56Fmoc-NH-PEG-NHS ........................................................................ PEG1116 ............ 56Fmoc-NH-PEG-NHS ........................................................................ PEG1117 ............ 56Fmoc-NH-PEG-NHS ........................................................................ PEG1118 ............ 56

Fmoc-NH-PEG(12)-COOH ................................................................ PEG1080 .......... 54Fmoc-NH-PEG(16)-COOH ................................................................ PEG3180 ...........55Fmoc-NH-PEG(27)-COOH ............................................................... PEG1210 ............55Fmoc-O1Pen-OH ............................................................................. FAA1565 ............53Fmoc-O1Pen-ol ............................................................................... FAL3010 ........... 82Fmoc-O2Oc-NH-CH2-CH(OMe)2 ..................................................... FAA6580 .......... 82Fmoc-O2Oc-O2Oc-OH .................................................................... FAA1787.............53Fmoc-O2Oc-O2Oc-OPfp ................................................................. FAA6790 ...........53Fmoc-O2Oc-OH .............................................................................. FAA1435 ............53Fmoc-O2Oc-OPfp ........................................................................... FAA6020 ...........53Fmoc-TOTA*HCl .............................................................................. FNN1011 ........... 79Fmoc-TTDS-OH .............................................................................. FAA1568 ............53H-O2Oc-O2Oc-O2Oc-OH ................................................................ PEG2770 ........... 61H-O2Oc-O2Oc-OH .......................................................................... PEG1221 ............ 61H-O2Oc-OH .................................................................................... PEG2420 ........... 61H-O2Oc-OtBu*HCI .......................................................................... PEG2430 ........... 61H2N-[mPEG(4)-mPEG(10)]2............................................................ PEG0216 .......... 42H2N-[mPEG(4)]4 ............................................................................ PEG0173 ........... 42H2N-dPEG™(12)-O-DMT ................................................................. PEG1315 ........... 82H2N-dPEG™(12)-OH ....................................................................... PEG1310 ........... 82H2N-dPEG™(4)-OH ........................................................................ PEG1320 ........... 82H2N-dPEG™(8)-OH ........................................................................ PEG1340 .......... 82H2N-dPEG™(11)-NH2 ...................................................................... PEG1500 ..........80H2N-dPEG™(12)-CO-OtBu .............................................................. PEG1350........... 62H2N-dPEG™(12)-COOH .................................................................. PEG1345 ........... 62H2N-dPEG™(12)-NHNH-Boc ........................................................... PEG4240 .......... 79H2N-dPEG™(16)-CO-OtBu .............................................................. PEG3690 ......... 62H2N-dPEG™(16)-COOH .................................................................. PEG3320 .......... 62H2N-dPEG™(20)-CO-OtBu ............................................................. PEG3700 .......... 63H2N-dPEG™(20)-COOH ................................................................. PEG3330 .......... 62H2N-dPEG™(24)-CO-OtBu .............................................................. PEG1360 .......... 63H2N-dPEG™(24)-COOH .................................................................. PEG1355 ........... 63H2N-dPEG™(24)-OH ...................................................................... PEG3740 .......... 82H2N-dPEG™(36)-CO-OtBu ............................................................. PEG3710 ........... 63H2N-dPEG™(36)-COOH ................................................................. PEG3340 .......... 63H2N-dPEG™(36)-OH ...................................................................... PEG3750 .......... 82H2N-PEG(4)-[mdPEG™(24)]3 ......................................................... PEG3350 .......... 42H2N-dPEG™(4)-[mPEG(12)]3 .......................................................... PEG1325 ........... 42H2N-dPEG™(4)-CO-OtBu ............................................................... PEG1375 ............ 61H2N-dPEG™(4)-COOH ................................................................... PEG1370 ............ 61H2N-dPEG™(4)-NHNH-Boc ............................................................ PEG1335 ........... 79H2N-dPEG™(6)-CO-OtBu ............................................................... PEG1305........... 62H2N-dPEG™(6)-COOH ................................................................... PEG1300 ........... 61H2N-dPEG™(8)-CO-OtBu ............................................................... PEG1385 ........... 62H2N-dPEG™(8)-COOH ................................................................... PEG1380 .......... 62H2N-dPEG™(8)-NHNH-Boc ............................................................ PEG4230 .......... 79H2N-EG2-CO-OtBu ......................................................................... PEG1365 ............ 61H2N-PEG-alkyne ............................................................................ PEG2950.......... 88H2N-PEG-alkyne ............................................................................ PEG2960 ......... 88H2N-PEG-alkyne ............................................................................ PEG2970 .......... 88H2N-PEG-alkyne ............................................................................ PEG2980 ......... 88H2N-PEG-COOH*HCl ...................................................................... PEG1095 .......... 63H2N-PEG-COOH*HCl ...................................................................... PEG1096 .......... 63H2N-PEG-COOH*HCl ...................................................................... PEG1097 ........... 63H2N-PEG-N3 ................................................................................... PEG3000 ......... 94H2N-PEG-N3 ................................................................................... PEG3010 .......... 94H2N-PEG-N3 ................................................................................... PEG3020 ......... 94H2N-PEG-N3 ................................................................................... PEG3030 .......... 94H2N-PEG-NH2 ................................................................................ PEG1001 ...........80H2N-PEG-NH2 ................................................................................ PEG1002 ..........80H2N-PEG-NH2 ................................................................................ PEG1003 ..........80H2N-PEG-NH2 ................................................................................ PEG1004 ..........80H2N-PEG-NH2 ................................................................................ PEG1005 ..........80H2N-PEG-OH .................................................................................. PEG1006 .......... 83H2N-PEG-OH .................................................................................. PEG1007 .......... 83H2N-PEG-OH .................................................................................. PEG1008 .......... 83H2N-PEG-SH*HCl............................................................................ PEG1196 .......... 124H2N-PEG-SH*HCl............................................................................ PEG1197........... 124H2N-PEG-SH*HCl............................................................................ PEG1198 .......... 124H2N-PEG-STrt ................................................................................. PEG1026 ......... 124H2N-PEG-STrt ................................................................................. PEG1027 .......... 124H2N-PEG-STrt ................................................................................. PEG1028 ......... 124H2N-PEG(11)-N3 .............................................................................. PEG3040 ......... 93H2N-PEG(12)-N3 ............................................................................. PEG1081 ........... 93H2N-PEG(20)-NH2 .......................................................................... PEG1000 ..........80H2N-PEG(23)-N3 ............................................................................ PEG3070 .......... 93H2N-PEG(3)-N3 .............................................................................. PEG3060 ......... 93H2N-PEG(35)-N3 ............................................................................ PEG3080 ......... 93



H2N-mPEG(4)-[mPEG(4)]3 ............................................................. PEG2295 .......... 42H2N-PEG(4)-[mPEG(8)]3 ................................................................ PEG2315 ........... 42H2N-PEG(7)-N3............................................................................... PEG1087........... 93H2N-PEG(8)-N3 .............................................................................. PEG2350 .......... 93H2N-PEG(8)-NH2............................................................................ PEG1204 ..........80H2N-PEG(9)-N3 .............................................................................. PEG3050 ......... 93HO-dPEG™(16)-COOH .................................................................... PEG3720 ...........67HO-dPEG™(20)-COOH ................................................................... PEG3730 ...........67HO-dPEG™(4)-CO-OtBu ................................................................. PEG1535 ........... 66HO-dPEG™(8)-CO-OtBu ................................................................. PEG1540 .......... 66HO-PEG-CONH-NH-Boc .................................................................. PEG1029 ...........81HO-PEG-CONH-NH-Boc .................................................................. PEG1030 ...........81HO-PEG-CONH-NH-Boc .................................................................. PEG1031 ............81HO-PEG-COOH ............................................................................... PEG1092 ...........67HO-PEG-COOH ............................................................................... PEG1093 ...........67HO-PEG-COOH ............................................................................... PEG1094 ...........67HO-PEG-OH .................................................................................... PEG1010 .......... 143HO-PEG-OH .................................................................................... PEG1011 ........... 143HO-PEG-OH .................................................................................... PEG1012 .......... 143HO-PEG-OH .................................................................................... PEG1013 .......... 143HO-PEG-OH .................................................................................... PEG1014 .......... 143HO-PEG-SH .................................................................................... PEG1017 .......... 129HO-PEG-SH .................................................................................... PEG1018 .......... 129HO-PEG-SH .................................................................................... PEG1019 .......... 129HO-PEG-STrt ................................................................................... PEG1023 ......... 129HO-PEG-STrt ................................................................................... PEG1024 ......... 129HO-PEG-STrt ................................................................................... PEG1025 ......... 129HO-PEG(12)-CO-OtBu ...................................................................... PEG1090 .......... 66HO-PEG(12)-OH .............................................................................. PEG1015 .......... 143HO-PEG(24)-CO-tBu ........................................................................ PEG2365 ...........67HO-PEG(28)-OH ............................................................................. PEG1009 ......... 143HO-PEG(6)-CO-OtBu ....................................................................... PEG2355 .......... 66HO-PEG(8)-OH ............................................................................... PEG1016 .......... 143HOOC-dPEG™(28)-COOH ............................................................... PEG1465............ 71HOOC-PEG(4)-[mPEG(12)]3 ............................................................ PEG1490 .......... 43HOOC-dPEG™(16)-COOH ............................................................... PEG4140 .......... 70HOOC-dPEG™(20)-COOH ............................................................... PEG4150 ........... 71HOOC-dPEG™(24)-COOH ............................................................... PEG4160 ........... 71HOOC-dPEG™(6)-COOH ................................................................. PEG1450 .......... 69HOOC-dPEG™(8)-COOH ................................................................. PEG1475 ........... 70HOOC-PEG-COOH........................................................................... PEG1082 ...........72HOOC-PEG-COOH........................................................................... PEG1083 ...........72HOOC-PEG-COOH........................................................................... PEG1084 ...........72HOOC-PEG-COOH........................................................................... PEG1085 ...........72HOOC-PEG-COOH........................................................................... PEG1086 ...........72HOOC-PEG(12)-COOH ..................................................................... PEG1091 ........... 70HOOC-PEG(3)-COOH ...................................................................... PEG3170 ........... 69HOOC-PEG(4)-[mPEG(24)]3 ............................................................ PEG3240 .......... 43HOOC-PEG(4)-[mPEG(4)]3 ............................................................. PEG2305 .......... 43HOOC-PEG(4)-[mPEG(8)]3 ............................................................. PEG2325 .......... 43HOOC-PEG(4)-COOH ...................................................................... PEG1430 .......... 69HOOC-PEG(8)-SS-PEG(8)-COOH ..................................................... PEG1119 ............119HS-dPEG™(12)-COOH ..................................................................... PEG3440..........118HS-dPEG™(16)-COOH ..................................................................... PEG3450 ..........119HS-dPEG™(20)-COOH .................................................................... PEG3460 .........119HS-dPEG™(4)-COOH ...................................................................... PEG1970 ...........118HS-FA-PEG(12)-COOH ..................................................................... PEG2000 .........119HS-FA-PEG(28)-COOH .................................................................... PEG2005 .........119HS-FA-PEG(8)-OH ........................................................................... PEG2010 ......... 128HS-PEG-CONH-NH-Boc ................................................................... PEG1101 ........... 125HS-PEG-CONH-NH-Boc ................................................................... PEG1102 .......... 125HS-PEG-CONH-NH-Boc ................................................................... PEG1103 .......... 125HS-PEG-COOH ................................................................................ PEG1098 ......... 120HS-PEG-COOH ................................................................................ PEG1099 ......... 120HS-PEG-COOH ................................................................................ PEG1100 .......... 120HS-PEG-SH ..................................................................................... PEG1121 ........... 130HS-PEG-SH ..................................................................................... PEG1122 .......... 130HS-PEG-SH ..................................................................................... PEG1123 .......... 130HS-PEG-SH ..................................................................................... PEG1124 .......... 130HS-PEG-SH ..................................................................................... PEG1125 .......... 130HS-PEG(8)-COOH ........................................................................... PEG1120 ...........118I-PEG-alkyne .................................................................................. PEG3090 ......... 88I-PEG-alkyne .................................................................................. PEG3100 .......... 88I-PEG-alkyne .................................................................................. PEG3110 ........... 88I-PEG-alkyne .................................................................................. PEG3120 .......... 88I-PEG-N3......................................................................................... PEG3130 ........... 98I-PEG-N3......................................................................................... PEG3140 .......... 98I-PEG-N3......................................................................................... PEG3150 .......... 98

I-PEG-N3......................................................................................... PEG3160 .......... 98Lipoamide-dPEG™(11)-biotin ......................................................... PEG3580.......... 113Lipoamide-dPEG™(11)-mal............................................................. PEG3560 .......... 114Lipoamide-dPEG™(12)-COOH ........................................................ PEG3520 .......... 113Lipoamide-dPEG™(12)-OMe........................................................... PEG3610 .......... 114Lipoamide-dPEG™(16)-COOH ........................................................ PEG3530 .......... 113Lipoamide-dPEG™(20)-COOH ....................................................... PEG3540 .......... 113Lipoamide-dPEG™(24)-OMe .......................................................... PEG3620 .......... 114Lipoamide-dPEG™(3)-biotin .......................................................... PEG3570 .......... 113Lipoamide-dPEG™(3)-mal ............................................................. PEG3550 .......... 114Lipoamide-dPEG™(4)-COOH ......................................................... PEG3500 ......... 113Lipoamide-dPEG™(4)-OMe ............................................................ PEG3590 .......... 114Lipoamide-dPEG™(8)-COOH ......................................................... PEG3510 .......... 113Lipoamide-dPEG™(8)-OMe ........................................................... PEG3600 ......... 114Mal-AMCHC-OH .............................................................................. MAA5400 ........ 131Mal-AMCHC-OSu ............................................................................ MAA1000 ......... 131Mal-beta-Ala-OSu .......................................................................... MAA1020 ......... 131mal-COOH...................................................................................... PEG2135 ........... 131mal-PEG(4)-[mPEG(12)]3 ................................................................ PEG1610 ........... 45mal-dPEG™(12)-NHNH-Boc ............................................................ PEG3890 ........ 136mal-dPEG™(12)-NHS ...................................................................... PEG1550 ..........133mal-dPEG™(16)-COOH ................................................................... PEG3860 .........133mal-dPEG™(16)-NHS ...................................................................... PEG3830 ..........133mal-dPEG™(20)-COOH .................................................................. PEG3870 ..........133mal-dPEG™(20)-NHS ..................................................................... PEG3840 .........133mal-dPEG™(24)-COOH................................................................... PEG1600 ......... 134mal-dPEG™(24)-NHS ..................................................................... PEG1565.......... 134mal-dPEG™(3)-mal ........................................................................ PEG1485 ......... 139mal-dPEG™(4)-COOH .................................................................... PEG1570 .......... 132mal-dPEG™(4)-NHNH-Boc ............................................................. PEG1580 ......... 136mal-dPEG™(4)-NHS ....................................................................... PEG1575 .......... 132mal-dPEG™(6)-COOH .................................................................... PEG3850......... 132mal-dPEG™(6)-NHS ....................................................................... PEG1585 ..........133mal-dPEG™(8)-COOH .................................................................... PEG1615 ...........133mal-dPEG™(8)-NHNH-Boc ............................................................. PEG3880 ........ 136mal-dPEG™(8)-NHS ....................................................................... PEG1590 ..........133mal-EG(2)-COOH ............................................................................ PEG1555 .......... 132mal-EG(2)-NHS .............................................................................. PEG1560 ......... 132mal-PEG-COOH .............................................................................. PEG1058 ......... 134mal-PEG-COOH .............................................................................. PEG1059 ......... 134mal-PEG-COOH .............................................................................. PEG1060 ......... 134mal-PEG-mal .................................................................................. PEG1126 .......... 139mal-PEG-mal .................................................................................. PEG1127 ........... 139mal-PEG-mal .................................................................................. PEG1128 .......... 139mal-PEG-mal .................................................................................. PEG1129 .......... 139mal-PEG-mal .................................................................................. PEG1130 .......... 139mal-PEG-NHS ................................................................................. PEG1061 .......... 134mal-PEG-NHS ................................................................................. PEG1062 ......... 134mal-PEG-NHS ................................................................................. PEG1063 ......... 134mal-PEG(12)-COOH ......................................................................... PEG2125 ...........133mal-PEG(12)-mal ............................................................................ PEG2085......... 139mal-PEG(27)-NHS ........................................................................... PEG1209 ......... 134mal-PEG(4)-[mPEG(24)]3 ............................................................... PEG3420 .......... 45mal-PEG(4)-[mPEG(4)]3 ................................................................. PEG2310 .......... 44mal-PEG(4)-[mPEG(8)]3 ................................................................. PEG2340 .......... 45MBS ............................................................................................... PEG2090 ......... 131MBz-PEG(12)-COOH ........................................................................ PEG2205 ......... 135MBz-PEG(12)-NHS ........................................................................... PEG2210 ......... 135MBz-PEG(24)-COOH ....................................................................... PEG2215 .......... 135MBz-PEG(24)-NHS .......................................................................... PEG2220 ......... 135MBz-PEG(4)-COOH ......................................................................... PEG2185.......... 135MBz-PEG(4)-NHS ............................................................................ PEG2190 ......... 135MBz-PEG(8)-COOH ......................................................................... PEG2195 ......... 135MBz-PEG(8)-NHS ............................................................................ PEG2200 ........ 135MeO-dPEG™(11)-O-CO-NHS ............................................................ PEG1645 ...........74MeO-dPEG™(12)-mal ..................................................................... PEG1665 ..........137MeO-dPEG™(12)-N3 ....................................................................... PEG1660 .......... 95MeO-dPEG™(12)-NH2..................................................................... PEG1655 ........... 84MeO-dPEG™(12)-NHS .................................................................... PEG1890 ...........74MeO-dPEG™(12)-SH ....................................................................... PEG3490......... 126MeO-dPEG™(15)-NH2..................................................................... PEG3290 .......... 84MeO-dPEG™(15)-O-CO-NHS ........................................................... PEG3390 ...........74MeO-dPEG™(15)-OH ...................................................................... PEG3250 ......... 145MeO-dPEG™(16)-NHS .................................................................... PEG1895 ...........75MeO-dPEG™(19)-O-CO-NHS ........................................................... PEG3400 ..........75MeO-dPEG™(19)-OH ...................................................................... PEG3260 ......... 145MeO-dPEG™(23)-O-CO-NHS .......................................................... PEG3410 ...........75MeO-dPEG™(23)-OH ...................................................................... PEG3270 ......... 145

NAME CODE PAGENAME CODE PAGE



MeO-dPEG™(24)-COOH ................................................................. PEG1635 ............75MeO-dPEG™(24)-mal ..................................................................... PEG1675 ...........137MeO-dPEG™(24)-N3 ...................................................................... PEG1710 ........... 95MeO-dPEG™(24)-NH2 .................................................................... PEG1670 ........... 84MeO-dPEG™(24)-NHS .................................................................... PEG1900 ...........75MeO-dPEG™(3)-COOH ................................................................... PEG1620 ...........73MeO-dPEG™(3)-NHS ...................................................................... PEG1880 ...........73MeO-dPEG™(3)-O-CO-NHS ............................................................ PEG1680 ...........74MeO-dPEG™(36)-mal .................................................................... PEG3360 ..........137MeO-dPEG™(36)-N3 ...................................................................... PEG3430 .......... 95MeO-dPEG™(36)-NH2 .................................................................... PEG3300 .......... 84MeO-dPEG™(36)-OH ..................................................................... PEG3280......... 145MeO-dPEG™(37)-COOH ................................................................. PEG3210 ...........75MeO-dPEG™(37)-NHS .................................................................... PEG3190 ...........75MeO-dPEG™(4)-N3 ........................................................................ PEG1690 .......... 95MeO-dPEG™(4)-NH2 ...................................................................... PEG1685 .......... 84MeO-dPEG™(4)-SH ........................................................................ PEG3470 ......... 126MeO-dPEG™(4)-Tos ........................................................................ PEG1695 ......... 144MeO-dPEG™(48)-mal .................................................................... PEG3370 ..........137MeO-dPEG™(48)-NH2 ................................................................... PEG3310 .......... 84MeO-dPEG™(49)-COOH ................................................................. PEG3220 ...........75MeO-dPEG™(49)-NHS.................................................................... PEG3200 ..........75MeO-dPEG™(7)-O-CO-NHS ............................................................ PEG3380 ...........74MeO-dPEG™(7)-Tos ........................................................................ PEG3820......... 144MeO-dPEG™(8)-COOH ................................................................... PEG1625............74MeO-dPEG™(8)-N3 ........................................................................ PEG1705 ........... 95MeO-dPEG™(8)-NH2 ..................................................................... PEG1700 .......... 84MeO-dPEG™(8)-NHS ..................................................................... PEG1885 ...........74MeO-dPEG™(8)-SH ........................................................................ PEG3480 ........ 126MeO-EG(2)-Tos ............................................................................... PEG1720 .......... 144MeO-EPr-COOH .............................................................................. PEG1630 ...........73MeO-EPr-NHS ................................................................................. PEG1905 ...........73MeO-PEG-alkyne ............................................................................ PEG2800 ..........87MeO-PEG-alkyne ............................................................................ PEG2810 ...........87MeO-PEG-alkyne ............................................................................ PEG2820...........87MeO-PEG-alkyne ............................................................................ PEG2830 ...........87MeO-PEG-alkyne ............................................................................ PEG2840 ..........87MeO-PEG-Br ................................................................................... PEG1131 ........... 142MeO-PEG-Br ................................................................................... PEG1132 .......... 142MeO-PEG-Br ................................................................................... PEG1133........... 142MeO-PEG-Br ................................................................................... PEG1134 .......... 142MeO-PEG-Br ................................................................................... PEG1135 .......... 142MeO-PEG-CHO ............................................................................... PEG1141 ............147MeO-PEG-CHO ............................................................................... PEG1142 ...........147MeO-PEG-CHO ............................................................................... PEG1143 ...........147MeO-PEG-CHO ............................................................................... PEG1144 ...........147MeO-PEG-CHO ............................................................................... PEG1145 ...........147MeO-PEG-COOH ............................................................................. PEG1157 .............76MeO-PEG-COOH ............................................................................. PEG1158 ............76MeO-PEG-COOH ............................................................................. PEG1159 ............76MeO-PEG-COOH ............................................................................. PEG1160 ............76MeO-PEG-COOH ............................................................................. PEG1161 .............76MeO-PEG-mal ................................................................................ PEG1146 .......... 138MeO-PEG-mal ................................................................................ PEG1147 ........... 138MeO-PEG-mal ................................................................................ PEG1148 .......... 138MeO-PEG-mal ................................................................................ PEG1149 .......... 138MeO-PEG-mal ................................................................................ PEG1150 .......... 138MeO-PEG-N3 .................................................................................. PEG1219 ........... 96MeO-PEG-N3 .................................................................................. PEG1225 ........... 96MeO-PEG-N3 .................................................................................. PEG2040 ......... 96MeO-PEG-N3 .................................................................................. PEG2045 .......... 96MeO-PEG-N3 .................................................................................. PEG2050 ......... 96MeO-PEG-NH2 ............................................................................... PEG1151 ............ 85MeO-PEG-NH2 ............................................................................... PEG1152 ........... 85MeO-PEG-NH2 ............................................................................... PEG1153 ........... 85MeO-PEG-NH2 ............................................................................... PEG1154 ........... 85MeO-PEG-NH2 ............................................................................... PEG1155 ........... 85MeO-PEG-NHS ............................................................................... PEG1162 ............76MeO-PEG-NHS ............................................................................... PEG1163 ............76MeO-PEG-NHS ............................................................................... PEG1164 ............76MeO-PEG-NHS ............................................................................... PEG1165 ............76MeO-PEG-NHS ............................................................................... PEG1166 ............76MeO-PEG-O-CO-NHS ...................................................................... PEG1202 ...........76MeO-PEG-OH ................................................................................. PEG1033 .......... 145MeO-PEG-OH ................................................................................. PEG1034 ......... 145MeO-PEG-OH ................................................................................. PEG1035.......... 145MeO-PEG-OH ................................................................................. PEG1036 ......... 145MeO-PEG-OH ................................................................................. PEG1037 .......... 145

MeO-PEG-OMs ............................................................................... PEG1218 .......... 145MeO-PEG-OPSS .............................................................................. PEG4745 ..........127MeO-PEG-OPSS .............................................................................. PEG4750 ..........127MeO-PEG-OPSS .............................................................................. PEG4755 ..........127MeO-PEG-OPSS .............................................................................. PEG4760 ..........127MeO-PEG-OPSS .............................................................................. PEG4765 ..........127MeO-PEG-SH .................................................................................. PEG1168 ...........127MeO-PEG-SH .................................................................................. PEG1169 ...........127MeO-PEG-SH .................................................................................. PEG1170 ...........127MeO-PEG-SH .................................................................................. PEG1171 ............127MeO-PEG-SH .................................................................................. PEG1172 ............127MeO-PEG-Si(OMe)3 ........................................................................ PEG4790 ......... 140MeO-PEG-Si(OMe)3 ........................................................................ PEG4795 ......... 140MeO-PEG-Si(OMe)3 ........................................................................ PEG4800 ........ 140MeO-PEG-Si(OMe)3 ........................................................................ PEG4805 ........ 140MeO-PEG(11)-OH ............................................................................ PEG1038 ......... 144MeO-PEG(11)-PrCHO ....................................................................... PEG2335 ......... 146MeO-PEG(12)-COOH ....................................................................... PEG1156 ............74MeO-PEG(16)-COOH ....................................................................... PEG2370 ...........74MeO-PEG(24)-CHO ......................................................................... PEG2180 ......... 146MeO-PEG(4)-CHO ........................................................................... PEG2170 .......... 146MeO-PEG(4)-mal ............................................................................ PEG2375 ..........137MeO-PEG(4)-OH ............................................................................. PEG2155 .......... 144MeO-PEG(7)-NH2 ........................................................................... PEG1730 ........... 84MeO-PEG(7)-OH ............................................................................. PEG1032.......... 144MeO-PEG(7)-SH .............................................................................. PEG1167 .......... 126MeO-PEG(7)-SS-PEG(7)-OMe .......................................................... PEG1195 .......... 126MeO-PEG(8)-CHO ........................................................................... PEG2175 .......... 146MeO-PEG(8)-mal ............................................................................ PEG2380 ..........137Mmt-NH-dPEG™(12)-TFP ................................................................ PEG4520 .......... 58Mmt-NH-dPEG™(16)-TFP ................................................................ PEG4530 .......... 58Mmt-NH-dPEG™(20)-TFP ............................................................... PEG4540.......... 59Mmt-NH-dPEG™(24)-TFP ............................................................... PEG4550 .......... 59Mmt-NH-dPEG™(36)-TFP ............................................................... PEG4560 ......... 59Mmt-NH-dPEG™(4)-TFP ................................................................. PEG4500 ..........57Mmt-NH-dPEG™(8)-TFP ................................................................. PEG4510 .......... 58Mmt-NH-PEG(12)-CO-OPfp.............................................................. PEG2395 .......... 58Mmt-NH-PEG(12)-COOH ................................................................. PEG2270 .......... 58Mmt-NH-PEG(16)-CO-OPfp ............................................................. PEG2400.......... 58Mmt-NH-PEG(16)-COOH ................................................................. PEG2275 .......... 58Mmt-NH-PEG(24)-CO-OPfp ............................................................. PEG2405 .......... 59Mmt-NH-PEG(24)-COOH ................................................................. PEG2280.......... 59Mmt-NH-PEG(4)-CO-OPfp ............................................................... PEG2385 ...........57Mmt-NH-PEG(4)-COOH .................................................................. PEG2160 ...........57Mmt-NH-PEG(8)-CO-OPfp .............................................................. PEG2390 .......... 58Mmt-NH-PEG(8)-COOH .................................................................. PEG2265 ...........57Mmt-S-dPEG™(12)-COOH ............................................................... PEG4600 .........119Mmt-S-dPEG™(16)-COOH ............................................................... PEG4610 ..........119Mmt-S-dPEG™(20)-COOH .............................................................. PEG4620 .........119Mmt-S-dPEG™(4)-COOH ................................................................ PEG1740 ...........118Mmt-S-dPEG™(8)-COOH ................................................................ PEG1735 ...........118Mmt-TTDS-OH ................................................................................ MAA1010 ...........57MP-EDA*TFA .................................................................................. PEG2105 ......... 136Mtt-O2Oc-OH*DEA ......................................................................... PEG4650 ..........57N3-dPEG™(12)-NHS ........................................................................ PEG1395 ............97N3-dPEG™(8)-NHS ......................................................................... PEG1405 ...........97N3-dPEG™(12)-COOH ..................................................................... PEG4180 ...........97N3-dPEG™(12)-OH.......................................................................... PEG1390 .......... 94N3-dPEG™(24)-COOH .................................................................... PEG4190 ...........97N3-dPEG™(24)-OH ......................................................................... PEG3770 .......... 95N3-dPEG™(36)-OH ......................................................................... PEG3780 .......... 95N3-dPEG™(4)-NHS ......................................................................... PEG1400 .......... 96N3-dPEG™(4)-OH ........................................................................... PEG3760 .......... 94N3-dPEG™(8)-COOH ...................................................................... PEG4170 ............97N3-O2Oc-O2Oc-OH*CHA ................................................................ PEG2790 ...........97N3-O2Oc-OH*CHA .......................................................................... PEG2780 .......... 96N3-PEG(20)-OH .............................................................................. PEG1220 .......... 94N3-PEG(4)-COOH ........................................................................... PEG2345 .......... 96N3-PEG(8)-OH ................................................................................ PEG1088 .......... 94N3-PEG(9)-COOH ........................................................................... PEG2015 ...........97N3-PGA(10)[mPEG(10)] ................................................................... PGA1610 ............ 41N3-PGA(10)[mPEG(20)] .................................................................. PGA1635 ........... 41N3-PGA(10)[Na] .............................................................................. PGA1120 ............27N3-PGA(100)[mPEG(10)]................................................................. PGA1625 ........... 41N3-PGA(100)[mPEG(20)] ................................................................ PGA1650 ........... 41N3-PGA(100)[Na] ........................................................................... PGA1135 ............27N3-PGA(20)[mPEG(10)] .................................................................. PGA1615 ............ 41N3-PGA(20)[mPEG(20)] ................................................................. PGA1640 ........... 41




N3-PGA(20)[Na] ............................................................................. PGA1125 ............27N3-PGA(200)[mPEG(10)] ................................................................ PGA1630 ........... 41N3-PGA(200)[mPEG(20)] ............................................................... PGA1655 ........... 41N3-PGA(200)[Na] ........................................................................... PGA1140 ............27N3-PGA(300)[Na] ........................................................................... PGA1145 ............27N3-PGA(400)[Na] ........................................................................... PGA1150 ............27N3-PGA(50)[mPEG(10)] .................................................................. PGA1620 ........... 41N3-PGA(50)[mPEG(20)] ................................................................. PGA1645 ........... 41N3-PGA(50)[Na] ............................................................................. PGA1130 ............27N3-PGA(800)[Na]........................................................................... PGA1155 ............27nBu-PGA(10)[mPEG(10)] ................................................................. PGA1460 ...........37nBu-PGA(10)[mPEG(20)] ................................................................ PGA1485 ...........37nBu-PGA(10)[Na] ............................................................................ PGA1000 ...........24nBu-PGA(10)[PEG2-N3(10)] ............................................................. PGA1260 .......... 30nBu-PGA(10)[PEG2-N3(10)] ............................................................. PGA1260 ...........32nBu-PGA(10)[PEG2-N3(20)] ............................................................ PGA1285 ...........33nBu-PGA(10)[PEG7-N3(10)] ............................................................. PGA1360 ...........35nBu-PGA(10)[PEG7-N3(20)] ............................................................ PGA1385 ...........35nBu-PGA(10)[Prg(10)] ..................................................................... PGA1160 ........... 28nBu-PGA(10)[Prg(20)] ..................................................................... PGA1185 ........... 28nBu-PGA(10)[Prg(20)] ..................................................................... PGA1185 ............ 31nBu-PGA(100)[mPEG(10)] ............................................................... PGA1475 ............37nBu-PGA(100)[mPEG(20)] .............................................................. PGA1500 .......... 38nBu-PGA(100)[Na] ......................................................................... PGA1015 ............24nBu-PGA(100)[PEG2-N3(10)] .......................................................... PGA1275 ............33nBu-PGA(100)[PEG2-N3(20)] .......................................................... PGA1300 ...........33nBu-PGA(100)[PEG7-N3(10)] ........................................................... PGA1375 ............35nBu-PGA(100)[PEG7-N3(20)] .......................................................... PGA1400 ...........35nBu-PGA(100)[Prg(10)] ................................................................... PGA1175 ........... 28nBu-PGA(100)[Prg(10)] ................................................................... PGA1175 ........... 30nBu-PGA(100)[Prg(20)] ................................................................... PGA1200 .......... 29nBu-PGA(100)[Prg(20)] ................................................................... PGA1200 ........... 31nBu-PGA(20)[mPEG(10)] ................................................................ PGA1465 ...........37nBu-PGA(20)[mPEG(20)] ............................................................... PGA1490 ...........37nBu-PGA(20)[Na] ........................................................................... PGA1005 ...........24nBu-PGA(20)[PEG2-N3(10)] ............................................................ PGA1265 .......... 30nBu-PGA(20)[PEG2-N3(10)] ............................................................ PGA1265 ...........32nBu-PGA(20)[PEG2-N3(20)] ........................................................... PGA1290 ...........33nBu-PGA(20)[PEG7-N3(10)] ............................................................ PGA1365 ...........35nBu-PGA(20)[PEG7-N3(20)] ........................................................... PGA1390 ...........35nBu-PGA(20)[Prg(10)] ..................................................................... PGA1165 ........... 28nBu-PGA(20)[Prg(20)] .................................................................... PGA1190 ........... 28nBu-PGA(20)[Prg(20)] .................................................................... PGA1190 ............ 31nBu-PGA(200)[mPEG(10)] .............................................................. PGA1480 ...........37nBu-PGA(200)[mPEG(20)] ............................................................. PGA1505 .......... 38nBu-PGA(200)[Na] ......................................................................... PGA1020 ...........24nBu-PGA(200)[PEG2-N3(10)] .......................................................... PGA1280 ...........33nBu-PGA(200)[PEG2-N3(20)] ......................................................... PGA1305 ...........33nBu-PGA(200)[PEG7-N3(10)] .......................................................... PGA1380 ...........35nBu-PGA(200)[PEG7-N3(20)] ......................................................... PGA1405 ...........35nBu-PGA(200)[Prg(10)] ................................................................... PGA1180 ........... 28nBu-PGA(200)[Prg(10)] ................................................................... PGA1180 ............ 31nBu-PGA(200)[Prg(20)] .................................................................. PGA1205 .......... 29nBu-PGA(200)[Prg(20)] .................................................................. PGA1205 ........... 31nBu-PGA(300)[Na] ......................................................................... PGA1025 ...........24nBu-PGA(400)[Na] ......................................................................... PGA1030 ...........24nBu-PGA(50)[mPEG(10)] ................................................................ PGA1470............37nBu-PGA(50)[mPEG(20)] ............................................................... PGA1495 ...........37nBu-PGA(50)[Na] ........................................................................... PGA1010 ............24nBu-PGA(50)[PEG2-N3(10)] ............................................................ PGA1270........... 30nBu-PGA(50)[PEG2-N3(10)] ............................................................ PGA1270............33nBu-PGA(50)[PEG2-N3(20)] ........................................................... PGA1295 ...........33nBu-PGA(50)[PEG7-N3(10)] ............................................................ PGA1370 ............35nBu-PGA(50)[PEG7-N3(20)] ........................................................... PGA1395 ...........35nBu-PGA(50)[Prg(10)] ..................................................................... PGA1170 ........... 28nBu-PGA(50)[Prg(20)] .................................................................... PGA1195 ........... 29nBu-PGA(50)[Prg(20)] .................................................................... PGA1195 ............ 31nBu-PGA(800)[Na] ......................................................................... PGA1035 ...........24NHS-[mPEG(4)]4 ............................................................................ PEG0183 .......... 44NHS-DOODA-NHS .......................................................................... PEG4120 .......... 68NHS-dPEG™(4)-[mPEG(12)]3 .......................................................... PEG1840 .......... 44NHS-dPEG™(12)-NHS ..................................................................... PEG3980 ......... 70NHS-dPEG™(16)-NHS ..................................................................... PEG3990 ......... 70NHS-dPEG™(20)-NHS .................................................................... PEG4000 .......... 71NHS-dPEG™(24)-NHS .................................................................... PEG4010 ........... 71NHS-dPEG™(4)-NHNH-Boc ............................................................ PEG1855 ........... 49NHS-dPEG™(4)-NHS ...................................................................... PEG1435 ........... 69NHS-dPEG™(4)-NHS ...................................................................... PEG3960 ......... 69

NHS-dPEG™(6)-NHS ...................................................................... PEG3970 .......... 69NHS-dPEG™(8)-NHS ...................................................................... PEG1460 .......... 70NHS-PEG-alkyne ............................................................................ PEG2850.......... 89NHS-PEG-alkyne ............................................................................ PEG2860 ......... 89NHS-PEG-alkyne ............................................................................ PEG2870 .......... 89NHS-PEG-alkyne ............................................................................ PEG2880 ......... 89NHS-PEG-NHS ................................................................................ PEG1183 ............72NHS-PEG-NHS ................................................................................ PEG1184 ............72NHS-PEG-NHS ................................................................................ PEG1185 ............72NHS-PEG-NHS ................................................................................ PEG1186 ............72NHS-PEG-NHS ................................................................................ PEG1187.............72NHS-PEG(4)-[mPEG(24)]3 .............................................................. PEG3230 .......... 44NHS-PEG(4)-[mPEG(4)]3 ................................................................ PEG2300.......... 44NHS-PEG(4)-[mPEG(8)]3 ................................................................ PEG2320 .......... 44NHS-PEG(4)-CO-OBzl ..................................................................... PEG2115 ........... 69NHS-PEG(8)-SS-PEG(8)-NHS........................................................... PEG1188 ...........119NHS-PEG(NH-Boc)-alkyne .............................................................. PEG2900 ......... 90NHS-PEG(NH-Boc)-alkyne .............................................................. PEG2910 .......... 90NHS-PEG(NH-Boc)-alkyne .............................................................. PEG2920 .......... 90NHS-PEG(NH-Boc)-alkyne .............................................................. PEG2930 .......... 90NHS-TUDA-NHS .............................................................................. PEG4130 .......... 68Npt-PGA(10)[mPEG(10)] ................................................................. PGA1510 ........... 38Npt-PGA(10)[mPEG(20)] ................................................................. PGA1535........... 38Npt-PGA(10)[Na] ............................................................................ PGA1040 .......... 25Npt-PGA(10)[PEG2-N3(10)] ............................................................. PGA1310 ........... 34Npt-PGA(10)[PEG2-N3(20)] ............................................................. PGA1335 ........... 34Npt-PGA(10)[PEG7-N3(10)] ............................................................. PGA1410 ........... 36Npt-PGA(10)[PEG7-N3(20)] ............................................................. PGA1435........... 36Npt-PGA(10)[Prg(10)] ...................................................................... PGA1210 ........... 29Npt-PGA(10)[Prg(10)] ...................................................................... PGA1210 ............ 31Npt-PGA(10)[Prg(20)] ..................................................................... PGA1235 ........... 30Npt-PGA(10)[Prg(20)] ..................................................................... PGA1235 ............32Npt-PGA(100)[mPEG(10)] ............................................................... PGA1525........... 38Npt-PGA(100)[mPEG(20)]............................................................... PGA1550 .......... 39Npt-PGA(100)[Na] .......................................................................... PGA1055 .......... 25Npt-PGA(100)[PEG2-N3(10)] ........................................................... PGA1325 ........... 34Npt-PGA(100)[PEG2-N3(20)] .......................................................... PGA1350 .......... 34Npt-PGA(100)[PEG7-N3(10)] ........................................................... PGA1425 .......... 36Npt-PGA(100)[PEG7-N3(20)] ........................................................... PGA1450 .......... 36Npt-PGA(100)[Prg(10)] .................................................................... PGA1225........... 29Npt-PGA(100)[Prg(10)] .................................................................... PGA1225............32Npt-PGA(100)[Prg(20)] ................................................................... PGA1250 .......... 30Npt-PGA(100)[Prg(20)] ................................................................... PGA1250 ...........32Npt-PGA(20)[mPEG(10)] ................................................................. PGA1515 ........... 38Npt-PGA(20)[mPEG(20)] ................................................................ PGA1540 .......... 38Npt-PGA(20)[Na] ............................................................................ PGA1045 .......... 25Npt-PGA(20)[PEG2-N3(10)] ............................................................. PGA1315 ........... 34Npt-PGA(20)[PEG2-N3(20)] ............................................................ PGA1340 .......... 34Npt-PGA(20)[PEG7-N3(10)] ............................................................. PGA1415 ........... 36Npt-PGA(20)[PEG7-N3(20)] ............................................................ PGA1440 .......... 36Npt-PGA(20)[Prg(10)] ..................................................................... PGA1215 ........... 29Npt-PGA(20)[Prg(10)] ..................................................................... PGA1215 ............ 31Npt-PGA(20)[Prg(20)] ..................................................................... PGA1240 .......... 30Npt-PGA(20)[Prg(20)] ..................................................................... PGA1240 ...........32Npt-PGA(200)[mPEG(10)]............................................................... PGA1530 .......... 38Npt-PGA(200)[mPEG(20)] .............................................................. PGA1555........... 39Npt-PGA(200)[Na] ......................................................................... PGA1060 .......... 25Npt-PGA(200)[PEG2-N3(10)] .......................................................... PGA1330 .......... 34Npt-PGA(200)[PEG2-N3(20)] .......................................................... PGA1355 ........... 34Npt-PGA(200)[PEG7-N3(10)] ........................................................... PGA1430 .......... 36Npt-PGA(200)[PEG7-N3(20)] .......................................................... PGA1455 .......... 36Npt-PGA(200)[Prg(10)] ................................................................... PGA1230 .......... 29Npt-PGA(200)[Prg(10)] ................................................................... PGA1230 ...........32Npt-PGA(200)[Prg(20)] ................................................................... PGA1255........... 30Npt-PGA(200)[Prg(20)] ................................................................... PGA1255............32Npt-PGA(300)[Na] ......................................................................... PGA1065 .......... 25Npt-PGA(400)[Na] ......................................................................... PGA1070 .......... 25Npt-PGA(50)[mPEG(10)] ................................................................. PGA1520 .......... 38Npt-PGA(50)[mPEG(20)] ................................................................ PGA1545 .......... 38Npt-PGA(50)[Na] ............................................................................ PGA1050 .......... 25Npt-PGA(50)[PEG2-N3(10)]............................................................. PGA1320 .......... 34Npt-PGA(50)[PEG2-N3(20)] ............................................................ PGA1345........... 34Npt-PGA(50)[PEG7-N3(10)] ............................................................. PGA1420 .......... 36Npt-PGA(50)[PEG7-N3(20)] ............................................................ PGA1445 .......... 36Npt-PGA(50)[Prg(10)] ..................................................................... PGA1220 .......... 29Npt-PGA(50)[Prg(10)] ..................................................................... PGA1220 ...........32Npt-PGA(50)[Prg(20)] ..................................................................... PGA1245 ........... 30Npt-PGA(50)[Prg(20)] ..................................................................... PGA1245 ............32

NAME CODE PAGENAME CODE PAGE



Npt-PGA(800)[Na] ......................................................................... PGA1075........... 25OHC-PEG-CHO ................................................................................ PEG1178 ...........147OHC-PEG-CHO ................................................................................ PEG1179 ...........147OHC-PEG-CHO ................................................................................ PEG1180 ...........147OHC-PEG-CHO ................................................................................ PEG1181 ............147OHC-PEG-CHO ................................................................................ PEG1182 ...........147OPSS-dPEG™(16)-COOH................................................................. PEG3930 ......... 122OPSS-dPEG™(16)-NHS ................................................................... PEG3900 ........ 122OPSS-dPEG™(20)-COOH ................................................................ PEG3940 ........ 122OPSS-dPEG™(20)-NHS................................................................... PEG3910 ......... 123OPSS-dPEG™(36)-COOH ................................................................ PEG3950 ......... 123OPSS-dPEG™(36)-NHS ................................................................... PEG3920 ......... 123OPSS-PEG-NHS .............................................................................. PEG1215 .......... 123OPSS-PEG-NHS .............................................................................. PEG1216 .......... 123OPSS-PEG-NHS .............................................................................. PEG1217 ........... 123OPSS-PEG-NHS .............................................................................. PEG4720 ......... 123OPSS-PEG-OPSS ............................................................................. PEG4715 .......... 130OPSS-PEG-OPSS ............................................................................. PEG4725 ......... 130OPSS-PEG-OPSS ............................................................................. PEG4730 ......... 130OPSS-PEG-OPSS ............................................................................. PEG4735 ......... 130OPSS-PEG-OPSS ............................................................................. PEG4740 ......... 130OPSS-PEG(12)-COOH ...................................................................... PEG2245 ......... 122OPSS-PEG(12)-NHS ......................................................................... PEG2250 ......... 122OPSS-PEG(24)-COOH...................................................................... PEG2255 ......... 123OPSS-PEG(24)-NHS ........................................................................ PEG2260 ......... 123OPSS-PEG(4)-COOH ....................................................................... PEG2225 ......... 122OPSS-PEG(4)-NHS .......................................................................... PEG2230 ......... 122OPSS-PEG(8)-COOH ....................................................................... PEG2235 ......... 122OPSS-PEG(8)-NHS .......................................................................... PEG2240 ......... 122Palm3-Cys-PEG-OH ......................................................................... PEG0306 ......... 45Palm3-Cys-PEG-OH ......................................................................... PEG0506 ......... 45PEG-Pentrimer-G1-(Boc-NH+4xN3) ................................................. DDN2060 ....... 149PEG-Pentrimer-G1-(N3+4xBoc-NH) ................................................. DDN2030 ....... 148PEG-Pentrimer-G1-(N3+4xNH2) ...................................................... DDN2040 ....... 149PEG-Pentrimer-G1-(NH2+4xBoc-NH) .............................................. DDN2000 ....... 148PEG-Pentrimer-G1-(NH2+4xN3) ...................................................... DDN2050 ....... 149PEG-Pentrimer-G1-(TFA-NH+4xBoc-NH).......................................... DDN2020 ....... 148PEG-Pentrimer-G1-(Z-NH+4xBoc-NH) ............................................. DDN2010 ........ 148Pfp-DOODA-Pfp .............................................................................. PEG4020 ......... 68Pfp-dPEG™(12)-Pfp ......................................................................... PEG4080 ......... 70Pfp-dPEG™(16)-Pfp ......................................................................... PEG4090 .......... 71Pfp-dPEG™(20)-Pfp ........................................................................ PEG4100 ........... 71Pfp-dPEG™(3)-Pfp .......................................................................... PEG4040 ......... 69Pfp-dPEG™(4)-Pfp .......................................................................... PEG4050 ......... 69Pfp-dPEG™(6)-Pfp .......................................................................... PEG4060 ......... 70Pfp-dPEG™(8)-Pfp .......................................................................... PEG4070 .......... 70Pfp-TUDA-Pfp ................................................................................. PEG4030 ......... 68Phth-NO-dPEG™(12)-NHS .............................................................. PEG4630...........55Prg-PGA(10)[mPEG(10)] .................................................................. PGA1560 .......... 39Prg-PGA(10)[mPEG(20)].................................................................. PGA1585 .......... 40Prg-PGA(10)[Na] ............................................................................. PGA1080 .......... 26Prg-PGA(100)[mPEG(10)] ................................................................ PGA1575 ........... 39Prg-PGA(100)[mPEG(20)] ............................................................... PGA1600 .......... 40Prg-PGA(100)[Na] ........................................................................... PGA1095 .......... 26Prg-PGA(20)[mPEG(10)].................................................................. PGA1565 .......... 39Prg-PGA(20)[mPEG(20)] ................................................................. PGA1590 .......... 40Prg-PGA(20)[Na] ............................................................................ PGA1085 .......... 26Prg-PGA(200)[mPEG(10)] ............................................................... PGA1580 .......... 39Prg-PGA(200)[mPEG(20)] ............................................................... PGA1605 .......... 40Prg-PGA(200)[Na] .......................................................................... PGA1100........... 26Prg-PGA(300)[Na] .......................................................................... PGA1105 ........... 26Prg-PGA(400)[Na] .......................................................................... PGA1110 ........... 26Prg-PGA(50)[mPEG(10)].................................................................. PGA1570 .......... 39Prg-PGA(50)[mPEG(20)] ................................................................. PGA1595 .......... 40Prg-PGA(50)[Na] ............................................................................ PGA1090 .......... 26Prg-PGA(800)[Na] .......................................................................... PGA1115 ............ 26Propargyl amine ............................................................................ PEG2755 ...........87Propargyl-NHS ............................................................................... PEG1935 ............87Rhodamine B-dPEG™(4)-COOH ..................................................... PEG1545 ............77SS-Dendrimer-G1-(OH)2 ................................................................. DDN1300 ........ 155SS-Dendrimer-G1-Acetonide ........................................................... DDN1350 ........ 155SS-Dendrimer-G2-(Acetonide)2 ...................................................... DDN1360 ........ 155SS-Dendrimer-G2-(OH)4................................................................. DDN1310 ......... 155SS-Dendrimer-G3-(Acetonide)4 ...................................................... DDN1370 ......... 156SS-Dendrimer-G3-(OH)8 ................................................................ DDN1320 ........ 156SS-Dendrimer-G4-(Acetonide)8...................................................... DDN1380 ........ 156SS-Dendrimer-G4-(OH)16 ............................................................... DDN1330......... 156SS-Dendrimer-G5-(Acetonide)16 .................................................... DDN1390 ........ 156

SS-Dendrimer-G5-(OH)32 ............................................................... DDN1340 ........ 156Stea-O2Oc-OH................................................................................ PEG1203 ............73tBu-O2C-PEG(12)-COOH .................................................................. PEG1189 ............ 71Tfp-dPEG™(24)-Tfp ......................................................................... PEG4110 ............ 71TODA ............................................................................................. PEG2025 ...........73Trt-S-dPEG™(4)-COOH ................................................................... PEG1980 ..........118Trt-S-PEG-NHS ................................................................................ PEG1199 .......... 120Trt-S-PEG-NHS ................................................................................ PEG1200 ......... 120Trt-S-PEG-NHS ................................................................................ PEG1201 .......... 120TUDA ............................................................................................. PEG2030 .......... 68Z-NH-dPEG™(3)-NH2 ..................................................................... PEG1745 ...........80Z-NH-dPEG™(12)-COOH ................................................................. PEG1785 ........... 64Z-NH-dPEG™(16)-COOH ................................................................. PEG4570 .......... 64Z-NH-dPEG™(20)-COOH ................................................................ PEG4580 ......... 64Z-NH-dPEG™(24)-COOH ................................................................. PEG1790 .......... 65Z-NH-dPEG™(36)-COOH ................................................................ PEG4590 ......... 65Z-NH-dPEG™(4)-COOH .................................................................. PEG1495........... 64Z-NH-dPEG™(6)-COOH .................................................................. PEG1795 ........... 64Z-NH-dPEG™(8)-COOH .................................................................. PEG1800 .......... 64Z-O1Pen-OH .................................................................................... PEG4710........... 64Z-O2Oc-OH*DCHA .......................................................................... ZAA1186 ........... 64




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other publications from Iris Biotech:

Disulfide bridges are an important structural element in many proteins and peptides. This brochure is a guideline how to plan and execute the Synthesis of Cyclic Peptides with one or several disulfide bridges.

Very sensitive and highly specific high turnover cytochro-me P450 substrates for Drug Interaction studies and drug metabolites like glucuronides.

Make sure you get your copy of the latest edition of our Catalogue with over 5000 compounds for peptide syn-thesis, solid phase chemistry, drug delivery technologies (PEG, PAS, PGA) and many natural compounds, enzyme substrates and related reagents for biochemistry.


d ru G I n t E r aC t I o n





C yC l I C p E pt I d E s


Brochure for Click Chemistry containing over 200 dif-ferent Azido and Alkyne Compounds for drug discovery, drug delivery and diagnostics.


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pGa – pEGylation – pasylation – dendrimers

natural products, Enzymes & Enzyme substrates, Carbohydrates & Fluorophores

for molecular Biology, microbiology, Biochemistry & diagostics

Custom synthesis of pharmaceutical Intermediates & Building Blocks

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