Molecular Formula | C25H35NO4S |
Molar Mass | 445.61 |
Density | 1.21 |
Boling Point | 640.5±55.0 °C(Predicted) |
pKa | 3.67±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | VX-222 binds to the segment II allosteric pocket of HCV RNA-dependent RNA polymerase. VX-222 selective inhibition of HCV NS5B genotypes 1a and 1b as non-competitive inhibitors, with IC50 of 0.94 and 1.2 μm for NS5B 2a and human DNA polymerase, respectively. VX-222 selectively suppressed HCV genotypes 1a and 1b with EC50 of 22.3 and 11.2 nM, respectively. The latest study showed that VX-222 of the inhibition of 1b/Con1 HCV sub gene replicon, EC50 was 5nm. VX-222 preferentially inhibits primer-dependent RNA synthesis with no or very little inhibitory effect on restarted RNA synthesis. |
In vivo study | VCH-222 acts on mice and dogs, showing good drug kinetic spectrum, including low body clearance ability and excellent biological oral effectiveness, and good ADME ability. VCH-222 biotransformation by some enzymes (CYP1A1, 2A6, 2B6, 2C8, CYP 3A4, UGT1A3), good transport in the liver, secretion in the bile, alternatively, a gluconic acid adduct is formed. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.244 ml | 11.22 ml | 22.44 ml |
5 mM | 0.449 ml | 2.244 ml | 4.488 ml |
10 mM | 0.224 ml | 1.122 ml | 2.244 ml |
5 mM | 0.045 ml | 0.224 ml | 0.449 ml |