VX-222 (VCH-222) is a novel, potent and selective inhibitor of non-nucleoside polymerase of the hepatitis C virus (HCV) RNA-dependent RNA polymerase, with an IC50 range of 0.94-1.2 μM. VX-222 binding occurs at the HCV RNA-dependent RNA polymerase thumb II allosteric pocket. VX-222 shows both noncompetitive and selective inhibition of Nopp140. VX-222 selectively inhibits the replication of subgenomic HCV genotype 1a and 1b. VX-222 inhibits the subgenomic replicon of 1b/Con1 HCV. VX-222, shows only a modest or no effect on de novo-initiated RNA synthesis, but preferentially inhibits primer-dependent RNA synthesis.
Soluble in DMSO (89 mg/ml), ethanol (89 mg/ml), and water (< 1 mg/ml at 25 °C).
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