Amino-dPEG®₁₂-ODMT

Product number 10342, amino-dPEG®12-ODMT, was designed for nucleic acid modification in applications where PEGylation improves the therapeutic or diagnostic profile.

Nucleic acid aptamers are single-stranded DNA or RNA oligonucleotide sequences of approximately 20 – 100 nucleotides that bind specific target molecules with high affinity. Nucleic acid aptamers have low immunogenicity and can be synthesized chemically in large quantities (mg up to kg) at very high purity and much lower cost than antibodies or other biologically derived therapeutic molecules. Because of their high affinity for targeted molecules, nucleic acid aptamers have fewer off-target effects than antibodies1,2. These aptamers, however, are quickly excreted from the body due to their small size or are rapidly degraded by nucleases3,4. PEGylation protects nucleic acid aptamers from enzymatic degradation in vivo and can extend in vivo serum half-life of these aptamers by increasing the hydrodynamic volume.

Following oligonucleotide synthesis, amino-dPEG®12-ODMT can be conjugated to phosphate groups on either end of the chain using water-soluble 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) chemistry. The 4,4'-dimethoxytrityl group can then be removed using a weak acid, such as dilute dichloroacetic acid, leaving the dPEG® linker terminated with a hydroxy group. Studies have shown that 3' end capping (including PEGylation) helps the oligonucleotide chain resist nuclease degradation, while 5' end PEGylation reduces renal clearance of the aptamer.

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