| Molecular Formula | C10H14FN3O4 |
| Molar Mass | 259.23 |
| Density | 1.67 |
| Melting Point | 216-218℃ |
| Boling Point | 482.4±55.0 °C(Predicted) |
| Solubility | DMSO |
| Appearance | Solid |
| Color | White to Light Brown |
| pKa | 12.86±0.70(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| Stability | Hygroscopic |
| Use | PSI-6130 is an HCV NS5B polymerase inhibitor |
| In vitro study | PSI-6130 exhibits potent and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase. Both PSI-6130 inhibit HCV GT-1b (Con1 strain) and GT-1a (H77 strain) subgenomic RNA replication, with mean EC 50 values of 0.51 and 0.30 μM, respectively. PSI-6130 inhibits 40% human serum with EC 50 of 0.51 μM. PSI-6130 inhibits HCV replication with a mean IC 50 of 0.6 μM, PSI-6130-TP inhibits HCV replicase with a mean IC 50 of 0.34 μM. PSI-6130-TP inhibits recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3′-end of the negative strand of the HCV genome with an IC 50 of 0.13 μM and K i of 0.023 μM. |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.858 ml | 19.288 ml | 38.576 ml |
| 5 mM | 0.772 ml | 3.858 ml | 7.715 ml |
| 10 mM | 0.386 ml | 1.929 ml | 3.858 ml |
| 5 mM | 0.077 ml | 0.386 ml | 0.772 ml |
| biological activity | PSI-6130 is a highly effective, selective HCV NS5B polymerase inhibitor, which can inhibit HCV replication with an IC50 value of 0.6 μM. |
| target | IC50: 0.6 μM (HCV replication) |
| in vitro study | PSI-6130 exhibits potent and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase. Both PSI-6130 inhibit HCV GT-1b (Con1 STRAIN) and GT-1a (H77 STRAIN) subgenomic RNA replication, with mean EC 50 values of 0.51 and 0.30 μM, respectively. PSI-6130 inhibits 40% human serum with EC 50 of 0.51 μ m. PSI-6130 inhibits HCV replication with a mean IC 50 of 0.6 μ m, PSI-6130-TP inhibits HCV replicase with a mean IC 50 of 0.34 μ m. PSI-6130-TP inhibits recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3 '-end of the negative strand of the HCV local with an IC 50 of 0.13 μ m and K I of 0.023 μ m. |