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Asunaprevir

Cat. No. M2340
Asunaprevir Structure
Synonym:

BMS-650032

Size Price Availability Quantity
10mM*1mL In DMSO USD 480 In stock
5mg USD 200 In stock
10mg USD 330 In stock
50mg USD 880 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Asunaprevir (BMS-650032) is a potent hepatitis C virus (HCV) NS3 protease inhibitor for the treatment 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 recombinant enzymes representing genotypes 1a (H77) and 1b (J4L6S), respectively. In cell culture, asunaprevir (BMS-650032) inhibited replication of HCV replicons representing genotypes 1 and 4, with 50% effective concentrations (EC(50)s) ranging from 1 to 4 nM, and had weaker activity against genotypes 2 and 3 (EC(50), 67 to 1,162 nM). Asunaprevir at doses of 200 to 600 mg resulted in rapid HCV RNA decreases from the baseline; maximal mean changes in HCV RNA over time were 2.7 and 3.5 log(10) IU/ml in the SAD and MAD studies, respectively. Plasma and tissue exposures in vivo in several animal species indicated that asunaprevir displayed a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species). Asunaprevir (BMS-650032) is currently in phase III clinical trials.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 748.29
Formula C35H46ClN5O9S
CAS Number 630420-16-5
Purity >98%
Solubility DMSO
Storage at -20°C
References

The effect of hepatic impairment on the pharmacokinetics of asunaprevir, an HCV NS3 protease inhibitor.
Eley T, et al. Antivir Ther. 2014 Apr 7. PMID: 24704773.

The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, et al. J Med Chem. 2014 Mar 13;57(5):1730-52. PMID: 24564672.

Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032).
McPhee F, et al. Antimicrob Agents Chemother. 2012 Oct;56(10):5387-96. PMID: 22869577.

Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir.
McPhee F, et al. Antimicrob Agents Chemother. 2012 Jul;56(7):3670-81. PMID: 22508297.

Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C.
Pasquinelli C, et al. Antimicrob Agents Chemother. 2012 Apr;56(4):1838-44. PMID: 22290978.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Asunaprevir, BMS-650032 supplier, HCV Protease, inhibitors

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