MK-5172 is a novel NS3/4, a protease inhibitor for chronic HCV infection (Enzyme Ki for genotype1b, 2a, 2b and 3a at <0.02, 0.15, 0.02 and 0.7 nM, respectively). This agent has an attractive preclinical profile including high potency in vitro, significant liver exposure upon oral dosing, and potent inhibitory activity against viral variants that are resistant to other protease inhibitors in development. MK-5172 has also demonstrated anti-viral efficacy in a chimpanzee model of chronic HCV infection.
Molecular Weight | 766.9 |
Formula | C38H50N6O9S |
CAS Number | 1350514-68-9 |
Solubility (25°C) | DMSO 85 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
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