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 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.
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|
Merimepodib, also known as VX-497, is an orally bioavailable IMPDH inhibitor with broad spectrum antiviral activities.
Inarigivir soproxil, also known as SB 9200, is a novel agonist of innate immunity, which shows potent antiviral activity against resistant HCV variants.
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5 and 366 pM against genotype 6a.
Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50 values of 1 and 0.21 nM for HCV 1a and 1b, respectively.
Block lipid transport-1 (BLT-1) is a specific inhibitor of the SR-BI (Scavenger receptor, class B, type I) mediated lipid transfer.
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