产品
编 号:F529938
分子式:C18H26FN3O6
分子量:399.41
产品类型
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CAS No: 940908-79-2
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生物活性:
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.
体外研究:
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.