VX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection. While the protease inhibitors (telaprevir and boceprevir) are the directly-targeted anti-HCV agents furthest along in the development pipeline, HCV polymerase - an enzyme responsible for copying viral genetic material-is also a promising target. VX-222 is a novel non-nucleoside HCV NS5B polymerase inhibitor with potent in vitro activity.
Cell Experiment | |
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Cell lines | Huh7.5 cells |
Preparation method | Trypsinizing Huh7.5 cells harboring HCV RNA replicons and plating into 48-well plates at a concentration of 4 × 104 cells/well. Changing the medium and adding VX-222in 200 μL of complete medium the next day. 48 hours later, total RNA is extracted and viral RNAs are quantified by real-time reverse transcription-PCR (RT-PCR). The effective drug concentrations that reduced HCV RNA replicon levels by 50% (EC50) are calculated by nonlinear regression analysis with log curve fitting |
Concentrations | 0.01 nM -10 μM |
Incubation time | 48 hours |
Animal Experiment | |
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Animal models | Rats or dogs |
Formulation | Dissolved in 30% PEG |
Dosages | 5 mg/kg for rats or 10 mg/kg for dogs |
Administration | By oral gavage |
Molecular Weight | 445.61 |
Formula | C25H35NO4S |
CAS Number | 1026785-59-0 |
Solubility (25°C) | DMSO 80 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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