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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 | |
|---|---|
| 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 | |
|---|---|
| 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 |
| Related HCV Protease Products |
|---|
| Telaprevir
Telaprevir (VX-950) is a novel hepatitis C virus (HCV) NS3-4A protease inhibitor with IC50 of < 0.2 μM. |
| BMS-790052
BMS-790052 (Daclatasvir) is a first-in-class, nonstructural protein 5A (NS5A) replication complex inhibitor with an EC50 of 9-50 pM. |
| Elbasvir
Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) replication complex inhibitor, with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively. |
| Dasabuvir (ABT-333)
ABT-333 is a nonnucleoside NS5B polymerase inhibitor for the treatment of HCV infection. |
| Asunaprevir
Asunaprevir (BMS-650032) is a novel inhibitor of the hepatitis C virus enzyme serine protease NS3. |
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