GalNAc-siRNA Conjugates

GalNAc-siRNA Conjugates

N-Acetylgalactosamine (GalNAc) is an amino sugar derivative of galactose. It can be used as a targeting ligand in antisense oligonucleotides (ASO) and siRNA therapeutics.

The structure of GalNAc (CAS No. 1811-31-0) Figure 1. The structure of GalNAc (CAS No. 1811-31-0)

The asialoglycoprotein receptor (ASGR) is an ideal hepatocyte-specific candidate for targeted drug delivery due to its high capacity for substrate clearance from serum by receptor mediated endocytosis and its high expression on hepatocytes, and conserved across species. GalNAc binds to the ASGR and then resulting in rapid receptor mediated endocytosis. So, conjugation of GalNAc has become a major strategy for delivery of oligos to hepatocytes.

Multivalent GalNAc-siRNA conjugates, where the multivalent GalNAc cluster is attached to the 3'-end of the sense strand of siRNA, can elicit robust gene silencing in hepatocytes both in vitro and in vivo without the aid of drug delivery agents. GalNAc-siRNA conjugates have become a simple solution to the siRNA drug delivery to the liver and have shown improved tissue-specific delivery and efficacy in ASO and siRNA areas.

What we provide?

We provide GalNAc-siRNA conjugates with high quality. We can design and synthesis the siRNA based on the target gene, and our parent company BOC Sciences can provide high quality GalNAc, we can conjugate them to form GalNAc-siRNA conjugates.

How we do?

  • siRNA design, synthesis, purification, characterization
  • Conjugate siRNA and GalNAc
  • Characterization

Why choose us?

  • High quality raw materials
  • Free design
  • Experienced experts
    Strict QA and QC
  • Advanced analytical equipments
  • Professional technical support
  • 1 on 1 customer service
  • Competitive price
  • Fast delivery

Ref:

  1. Springer, A. D., & Dowdy, S. F. (2018). GalNAc-siRNA Conjugates: Leading the Way for Delivery of RNAi Therapeutics. Nucleic Acid Therapeutics, 28(3), 109–118.
  2. Willoughby, J. L. S., Chan, A., Sehgal, A., Butler, J. S., Nair, J. K., Racie, T., … Zimmermann, T. S. (2018). Evaluation of GalNAc-siRNA Conjugate Activity in Pre-clinical Animal Models with Reduced Asialoglycoprotein Receptor Expression. Molecular Therapy, 26(1), 105–114.
  3. Foster, D. J., Brown, C. R., Shaikh, S., Trapp, C., Schlegel, M. K., Qian, K., … Milstein, S. (2018). Advanced siRNA Designs Further Improve In Vivo Performance of GalNAc-siRNA Conjugates. Molecular Therapy, 26(3), 708–717.
* Only for research. Not suitable for any diagnostic or therapeutic use.
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