Chemren Bio-Engineering Co., Ltd.

Biological Activity of GS-9620

 

GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7(TLR-7) in chimpanzees with chronic HBV infection.
IC50 Value:
Target: TLR7
GS-9620 is a novel oral agonist of Toll-like receptor 7 (TLR7) in development for the treatment of chronic viral hepatitis [1]. TLR7 is a highly conserved innate immune receptor expressed primarily on plasmacytoid dendritic cells and B lymphocytes [2].
in vitro:
in vivo: Short-term oral administration of GS-9620 provided long-term suppression of serum and liver HBV DNA. The mean maximum reduction of viral DNA was 2.2 logs, which occurred within 1 week of the end of GS-9620 administration; reductions of >1 log persisted for months. Serum levels of HBV surface antigen and HBV e antigen, and numbers of HBV antigen-positive hepatocytes, were reduced as hepatocyte apoptosis increased. GS-9620 administration induced production of interferon-α and other cytokines and chemokines, and activated interferon-stimulated genes, natural killer cells, and lymphocyte subsets [1].  Induction of chemokines/cytokines and IFN-stimulated genes were seen at GS-9620 doses ≥2 mg, well below doses that induced serum IFN-α or led to clinical adverse events [2].
Clinical trial: A Study Evaluating GS-9620 in Treatment Naive Subjects With Chronic Hepatitis B. Phage1

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Chemical Information

M.Wt	410.51	Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Formula	C22H30N6O2
CAS No	1228585-88-3
Solubility	DMSO

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