HCV-371 is a potent and selective HCV NS5B polymerase inhibitor. HCV-371 displayed broad inhibitory activities against the NS5B RdRp enzyme, with 50% inhibitory concentrations ranging from 0.3 to 1.8 microM for 90% of the isolates derived from HCV genotypes 1a, 1b, and 3a. HCV-371 showed no inhibitory activity against a panel of human polymerases, including mitochondrial DNA polymerase gamma, and other unrelated viral polymerases, demonstrating its specificity for the HCV polymerase. Fluorescence binding studies show that HCV-371 binds the NS5B with an apparent dissociation constant of 150 nM, leading to high selectivity and lack of cytotoxicity in the antiviral assays. References: Gopalsamy A, Lim K, Ciszewski G, Park K, Ellingboe JW, Bloom J, Insaf S, Upeslacis J, Mansour TS, Krishnamurthy G, Damarla M, Pyatski Y, Ho D, Howe AY, Orlowski M, Feld B, O'Connell J. Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors. J Med Chem. 2004 Dec 16;47(26):6603-8. PubMed PMID: 15588095.
纯度:≥98%
CAS:675184-27-7