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. Ombitasvir has EC50s of 14.1 and 5.0 pM against genotype 1a-H77 and 1b-Con1 subgenomic replicons, respectively.
In GT1a, variants M28V, L31V, and H58D confers 58- to 243-fold resistance to Ombitasvir. Single variants M28T, Q30R, and Y93C/S confers 800- to 8965-fold resistance, while Y93H/N confers >40000-fold resistance to Ombitasvir.
Molecular Weight | 894.11 |
Formula | C50H67N7O8 |
CAS Number | 1258226-87-7 |
Solubility (25°C) | DMSO: ≥ 60 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.
[2] DeGoey DA, et al. J Med Chem. Discovery of ABT-267, a pan-genotypic inhibitor of HCV NS5A.
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