Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease. Vaniprevir is active against both the genotype 1 and genotype 2 NS3/4a protease enzymes. Vaniprevir (MK-7009) has good plasma exposure and excellent liver exposure in multiple species.
|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.
Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
McCauley JA, et al. J Med Chem. 2010 Mar 25;53(6):2443-63. PMID: 20163176.
|Related HCV Protease Products|
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.
Boceprevir (EBP-520, SCH503034) is an HCV protease inhibitor (Ki=14 nM) for the treatment of hepatitis C virus infection.
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