BMS-790052 is a first-in-class, nonstructural protein 5A (NS5A) replication complex inhibitor with an EC50 of 9-50 pM. It is one of the most potent inhibitors of HCV replication reported so far. BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with EC50 of 7–13 pM. Residue 30 of NS5A is an important site for BMS-790052-mediated resistance in the hybrid replicons. BMS-790052 was well tolerated in all dose groups, with adverse events occurring with a similar frequency in BMS-790052- and placebo-treated groups. BMS-7590052 is the first NS5A replication complex inhibitor with multiple dose proof-of-concept in clinic. At doses of 1-100 mg daily, BMS-790052 was well tolerated, had a PK profile supportive of once-daily dosing, and produced a rapid and substantial decrease in HCV-RNA levels in patients chronically infected with HCV genotype 1.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥100 mg/mL
Ethanol ≥100 mg/mL
Effect on HCV Replication by Combinations of Direct Acting Antivirals Including NS5A Inhibitor Daclatasvir.
Pelosi et al. Antimicrob Agents Chemother. 2012 Jul 30. PMID: 22850513.
Correlation between NS5A Dimerization and Hepatitis C Virus Replication.
Lim et al. J Biol Chem. 2012 Aug 31;287(36):30861-73. PMID: 22801423.
Hepatitis C Virus NS5A Disrupts STAT1 Phosphorylation and Suppresses Type I Interferon Signaling.
Kumthip et al. J Virol. 2012 Aug;86(16):8581-91. PMID: 22674974.
Prevalence of hepatitis C virus variants resistant to NS3 protease inhibitors or the NS5A inhibitor (BMS-790052) in hepatitis patients with genotype 1b.
Suzuki et al. J Clin Virol. 2012 Aug;54(4):352-4. PMID: 22658798.
A sensitive and accurate liquid chromatography-tandem mass spectrometry method for quantitative determination of the novel hepatitis C NS5A inhibitor BMS-790052 (daclastasvir) in human plasma and urine.
Jiang et al. J Chromatogr A. 2012 Jul 6;1245:117-21. PMID: 22640838.
|Related HCV Protease Products|
Velpatasvir is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication.
Daclatasvir is a potent hepatitis C virus (HCV) NS5A protein inhibitor with picomolar EC50 value .
GS-9451, a novel hepatitis C virus (HCV) nonstructural 3/4a (NS3/4a) protease inhibitor, is highly active in patients infected with HCV genotype 1 (GT 1).
PSI-7977 (sofosbuvir) is an investigational nucleotide analog for treatment of chronic HCV infection.
BILN 2061 is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with IC50 of 3.0 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.