R-7128

Modify Date: 2024-01-01 19:21:23

R-7128 Structure
R-7128 structure
Common Name R-7128
CAS Number 940908-79-2 Molecular Weight 399.41400
Density N/A Boiling Point N/A
Molecular Formula C18H26FN3O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of R-7128


Mericitabine (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.

 Names

Name [(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-fluoro-4-methyl-3-(2-methylpropanoyloxy)oxolan-2-yl]methyl 2-methylpropanoate
Synonym More Synonyms

 R-7128 Biological Activity

Description Mericitabine (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.
Related Catalog
Target

HCV NS5B polymerase[1]

In Vitro Mericitabine (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 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 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. R-7128 is an oral cytidine nucleoside analog prodrug that exhibits strong antiviral effectiveness against the HCV polymerase across all HCV genotypes[3].
References

[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.

 Chemical & Physical Properties

Molecular Formula C18H26FN3O6
Molecular Weight 399.41400
Exact Mass 399.18100
PSA 123.73000
LogP 1.56050
Storage condition 2-8℃

 Synonyms

CS-0596
R-7128
Mericitabine (USAN/INN)
RG 7128
Mericitabine