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Asunaprevir

Cat. No. M2340
Asunaprevir Structure
Synonym:

BMS-650032

Size Price Availability Quantity
10mM*1mL in DMSO USD 230  USD230 In stock
5mg USD 140  USD140 In stock
10mg USD 225  USD225 In stock
25mg USD 450  USD450 In stock
50mg USD 680  USD680 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Eley T, et al. Antivir Ther. The effect of hepatic impairment on the pharmacokinetics of asunaprevir, an HCV NS3 protease inhibitor.

[2] Scola PM, et al. J Med Chem. The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.

[3] McPhee F, et al. Antimicrob Agents Chemother. Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032).

[4] McPhee F, et al. Antimicrob Agents Chemother. Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir.

[5] Pasquinelli C, et al. Antimicrob Agents Chemother. Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C.

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


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