Mericitabine | HY-10240

Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication.

IC50 & Target :

HCV NS5B polymerase

In Vitro:

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.

Molecular weight:

399.41

Formula:

C₁₈H₂₆FN₃O₆

SMILES:

O=C1N=C(C=CN1[C@@H]([C@@](C)([C@@H]2OC(C(C)C)=O)F)O[C@@H]2COC(C(C)C)=O)N

Storage: