Reagent for PEGylation

PEG reagents are useful for coupling to functional groups of biologically active agents such as proteins, antibody fragments, aptamers, peptides, and small molecules. The chemical attachment of PEG to these biologically active agents is referred to as “PEGylation”. PEGylation reaction conditions vary depending on the biological active, 0the desired site and degree of PEGylation, and the PEG reagent. Factors to consider in the choice of a PEG reagent are:

  • The desired functional point of attachment (amine, thiol, carboxyl, N-terminal, etc.);
  • Activity of the conjugate and its pharmacokinetics;
  • Multi-PEG species (PEGmers) and positional-PEG isomers;
  • Immunogenicity of the conjugate.

Utopbio offers PEGylation services for our customers who wish for us to develop a PEGylation process, analytical methods, or PEG-conjugate purification.

PEGylation: Reagent selection, conjugate linkage, and conjugate stability (under physiological conditions)

Carboxyl PEGylation

mPEG-amine and a coupling agent                                                     Amide (stable)  

Amine PEGylation

mPEG-NHS Esters (mPEG-SMB, -SPA or mPEG2-NHS)              Amide

mPEG-Double Ester (mPEG-CM-HBA-NHS)                                   Amide

N-terminal PEGylation

mPEG-ButyrALD and a reducing agent                                             Secondary amine (stable)

mPEG-OPTE                                                                                          Secondary amine (stable)

Thiol PEGylation

mPEG-Maleimide                                                                                  Sulfide (stable)

mPEG-OPSS                                                                                          Disulfide (can be reduced)

mPEG-SH                                                                                               Disulfide (can be reduced)

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