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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related HCV Protease Products |
---|
Hepatitis C Virus S5A/5B
Hepatitis C Virus S5A/5B is a synthetic peptide substrate. |
Ac-D-DGla-LI-Cha-C
Ac-D-DGla-LI-Cha-C is a potent HCV protease inhibitor peptide. |
Ac-EEVVAC-pNA
Ac-EEVVAC-pNA is a chromogenic substrate for a continuous spectrophotometric assay of HCV NS3 protease. |
Hepatitis Virus C NS3 Protease Inhibitor 2
Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM. |
Mipomersen
Mipomersen is a 20-base gapmer (antisense oligonucleotide) that inhibits apolipoprotein B (apoB) and lowers LDL, which can be used in studies related to hyperlipidemia. In addition, Mipomersen has anti-HCV activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.