Asunaprevir | CAS:630420-16-5

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Name:Asunaprevir; BMS-650032
Cat. No. :CS-0674
CAS No. :630420-16-5
Formula:C35H46ClN5O9S
M. Wt. : 748.29
Solubility:DMSO: ≥ 42.9 mg/mL

Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with the IC50 of 0.2 nM-3.5 nM.IC50 & Target: IC50: 0.2 nM-3.5 nM (HCV NS3 protease)In Vitro: In multiple experiments, populations of resistant colonies are markedly reduced when cells are treated with a combination of DCV and Asunaprevir[1]. Asunaprevir (ASV) inhibits the NS3 proteolytic activity of genotype 1a (H77 strain) and genotype 1b (J4L6S strain), with IC50s of 0.7 and 0.3 nM, respectively. The EC50s of ASV against replicons encoding the NS3 protease domains representing genotypes 1a, 1b, and 4a, range from 1.2 to 4.0 nM[2]. Replicon cells are maintained under selective pressure with asunaprevir at concentrations of 10 and 30 times the EC50 values (50 or 150 nM final concentrations, respectively). For genotype 1b resistance selection, replicon cells are maintained in the presence of asunaprevir at 10 or 30 times the EC50 values (30 or 90 nM final concentrations, respectively)[3]. Asunaprevir, administered at single or multiple doses of 200 to 600 mg twice daily, is generally well tolerated, achieving rapid and substantial decreases in HCV RNA levels in subjects chronically infected with genotype 1 HCV[4].In Vivo: Asunaprevir (ASV, 3-15 mg/kg, p.o.) displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species) in several animal species. Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50 observed with HCV genotype-1 replicons[2].

McPhee F, et al. Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir.Antimicrob Agents Chemother. 2012 Jul;56(7):3670-81. McPhee F, et al. Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032).Antimicrob Agents Chemother. 2012 Aug 6. Pelosi LA, et al. Effect on HCV Replication by Combinations of Direct Acting Antivirals Including NS5A Inhibitor Daclatasvir.Antimicrob Agents Chemother. 2012 Jul 30. Pasquinelli C, et al. Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C. Antimicrob Agents Chemother. 2012 Apr;56(4):1838-44.