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KI3555GS-9620QuoteQuote

Chemical Characteristic

Product NameGS-9620
CAS No.1228585-88-3
Molecular Weight 410.51
FormulaC22H30N6O2
Chemical Name6(5H)-Pteridinone, 4-amino-2-butoxy-7,8-dihydro-8-[[3-(1-pyrrolidinylmethyl)phenyl]methyl]
Smilesn1c(nc(c2NC(=O)CN(c12)Cc1cc(ccc1)CN1CCCC1)N)OCCCC
Chemical Structure

Biological activities

GS-9620 is a potent and selective agonist of Toll-like receptor 7(TLR7). GS-9620 is used for the treatment of chronic viral hepatitis.[1] In chronically hepatitis B virus (HBV) infected chimpanzees in vivo, GS-9620 administration reduces serum levels of HBV surface antigen and HBV e antigen, and numbers of HBV antigen-positive hepatocytes. Within 1 week of the end of GS-9620 administration ( 4 weeks at 1 mg/kg and, after a 1-week rest, for 4 weeks at 2 mg/kg), the mean maximum reduction of viral DNA is 2.2 logs, and reductions of >1 log persist for months. GS-9620 administration also induces production of interferon-α and other cytokines and chemokines (including IL-10, MCP-3 and IL-1α), and activates interferon-stimulated genes, natural killer cells, and lymphocyte subsets.[2]

References

[1] Roethle PA, et al. Identification and Optimization of Pteridinone Toll-like Receptor 7 (TLR7) Agonists for the Oral Treatment of Viral Hepatitis. J Med Chem. 2013, 56(18): 7324-7333.
[2] Lanford RE, et al. GS-9620, an oral agonist of Toll-like receptor-7, induces prolonged suppression of hepatitis B virus in chronically infected chimpanzees. Gastroenterology. 2013, 144(7): 1508-1517.

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