| Bioactivity | 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. | ||||||||||||
| Target | HCV NS5B polymerase | ||||||||||||
| Invitro | 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[2]. 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[3]. | ||||||||||||
| Name | Mericitabine | ||||||||||||
| CAS | 940908-79-2 | ||||||||||||
| Formula | C18H26FN3O6 | ||||||||||||
| Molar Mass | 399.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Le Pogam S, et al. Characterization of HCV quasispecies dynamics upon short term dual-therapy with the HCV NS5B nucleoside polymerase inhibitor mericitabine and the NS3/4 protease inhibitor danoprevir. Antimicrob Agents Chemother. 2012 Nov;56(11):5494-5 [2]. Soriano V, et al. Directly acting antivirals against hepatitis C virus. J Antimicrob Chemother. 2011 Aug;66(8):1673-86 [3]. Guedj J, et al. Hepatitis C viral kinetics with the nucleoside polymerase inhibitor mericitabine (RG7128). Hepatology. 2012 Apr;55(4):1030-7. |
Mericitabine
CAS: 940908-79-2 F: C18H26FN3O6 W: 399.41
Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator
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