R-7128

Research use only, not for human use.

The prodrug of PSI-6130, a potent, specific inhibitor of HCV RNA synthesis by inhibiting the NS5B RNA polymerase.

The prodrug of PSI-6130, a potent, specific inhibitor of HCV RNA synthesis by inhibiting the NS5B RNA polymerase.HCV Infection Phase 2 Discontinued.

Mericitabine (RG 7128; R-7128) is an oral prodrug of PSI-6130, a cytidine analogue. Pre-clinical observations demonstrated that PSI-6130 has an EC90 value of 4.6±2 μM in the HCV replicon assay. Mericitabine (RG 7128; R-7128) shows high specificity for HCV, minimal cytotoxicity and does not affect mitochondrial DNA. PSI-6130 is converted through phosphorylation by cellular kinases to an active 5′-triphosphate metabolite, which inhibits the NS5B RNA polymerase of HCV. Mericitabine (RG 7128; R-7128) demonstrates a relatively good safety profile and significant potency against HCV-1. Mericitabine is a first-in class nucleoside polymerase inhibitor (NPI), which requires intracellular uptake and phosphorylation to two active triphosphates.Mericitabine (RG 7128; R-7128) is an oral cytidine nucleoside analog prodrug that exhibits strong antiviral effectiveness against the HCV polymerase across all HCV genotypes.

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RG-7128 | Mericitabine | PSI-6130 diisobutyrate

Microbiology/Virology

HCV

HCV

Infection

HCV Infection

940908-79-2

399.4139

C18H26FN3O6

>98% (HPLC)

10 mM in DMSO

O=C(N=C(C=C1)N)N1[C@H](O2)[C@](C)(F)[C@H](OC(C(C)C)=O)[C@H]2COC(C(C)C)=O

Cytidine, 2'-deoxy-2'-fluoro-2'-methyl-, 3',5'-bis(2-methylpropanoate), (2'R)-

(-20℃)

With Ice Pack

≥ 2 years