| Bioactivity | PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM. | ||||||||||||
| Target | IC50: 0.6 μM (HCV replication) | ||||||||||||
| Invitro | 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 EC50 values of 0.51 and 0.30 μM, respectively. PSI-6130 inhibits 40% human serum with EC50 of 0.51 μM[1]. PSI-6130 inhibits HCV replication with a mean IC50 of 0.6 μM, PSI-6130-TP inhibits HCV replicase with a mean IC50 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 IC50 of 0.13 μM and Ki of 0.023 μM[2]. | ||||||||||||
| Name | PSI-6130 | ||||||||||||
| CAS | 817204-33-4 | ||||||||||||
| Formula | C10H14FN3O4 | ||||||||||||
| Molar Mass | 259.23 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Ali S, et al. Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479. Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69. [2]. Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):298 |
PSI-6130
CAS: 817204-33-4 F: C10H14FN3O4 W: 259.23
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.
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