IC50: 0.6 μM (HCV replication)

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.