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Asunaprevir (BMS-650032) is an effective hepatitis C virus (HCV) NS3 protease inhibitor for the study of hepatitis C virus infection. Asunaprevir competitively binds to the NS3/4A protease complex, with K(I) values of 0.4 and 0.24 nM against the 1a (H77) and 1B (J4L6S) genotypes, respectively. In cell culture, ASunaprevir (BMS-650032) inhibited replication of HCV replicons representing genotypes 1 and 4 at 50% effective concentration (EC(50)s) in the range of 1 -- 4 nM, but showed weak activity against genotypes 2 and 3 (EC(50), 67-1162 nM). Asunaprevir dose of 200-600 mg decreased HCV RNA levels from baseline; In the SAD and MAD studies, the maximum mean change in HCV RNA over time was 2.7 and 3.5 log(10) IU/ mL, respectively. Plasma and tissue exposures in several animal species have shown that Asunaprevir shows a hepatic tendency (liver-plasma ratio 40-359 times across species). Asunaprevir (BMS-650032) is currently in phase III clinical trials.
| Molecular Weight | 748.29 |
| Formula | C35H46ClN5O9S |
| CAS Number | 630420-16-5 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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