Toggle Nav

R-7128

In stock
Catalog No.
A3747
NS5B inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$386.00
In stock
5mg
$351.00
In stock
10mg
$477.00
In stock
50mg
$1,247.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

R-7128 is a selective nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase.

Hepatitis C virus (HCV) is an enveloped (+)-single stranded RNA virus, and the viral RNA is replicated in host cell via HCV's RNA-dependent RNA polymerase, which is the cause of hepatitis C and some cancer lymphomas.

R-7128 is a nucleotide triphosphate analog which is the substrate for HCV polymerase NS5B. Incorporation of R-7128 into nascent HCV RNA strongly decreased the efficiency of RNA elongation by RNA polymerase NS5B, leading to the termination of the nascent RNA product. It has been shown that R-7128 is able to inhibit the RNA synthesis of HCV in vitro [1].

32 patient infected with HCV genotype-1 was treated with R-7128 for 14 days with 750-mg or 1500-mg administered once (QD) or twice daily (BID), and the HCV RNA level was frequently measured. Initial decline of HCV RNA was generally slower than treatment with interferon-alpha or protease inhibitors but 12 patients showed a novel pattern of HCV RNA kinetics that the effectiveness in inhibiting viral production gradually increased over time to reach its final value. The final value was high with BID dose (mean 750-mg and 1500-mg: 98.0% and 99.8%, P=0.018) and significantly higher than in patients treated QD (mean QD vs BID: 90% vs 99%, P<10^-7) [2].

References:
[1] Ma H et al. , Characterization of the metabolic activation of Hepatitis C virus nucleoside inhibitor β-D-2′-Deoxy-2′-fluoro-2′-C-methylcytidine (PSI-6130) and identification of a novel active 5′-Triphosphate species. J Biol Chem. 2007, 282(41): 29812-20.
[2] Guedj J et al. , Hepatitis C viral kinetics with the nucleoside polymerase inhibitor mericitabine (RG7128). Hepatology. 2012, 55(4): 1030-1037.

Chemical Properties

StorageStore at -20°C
M.Wt399.41
Cas No.940908-79-2
FormulaC18H26FN3O6
SynonymsRG 7128; Mericitabine; PSI 6130 diisobutyrate
SolubilitySoluble in DMSO
Chemical 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
SDFDownload SDF
Canonical SMILESCC(C)C(=O)OCC1C(C(C(O1)N2C=CC(=NC2=O)N)(C)F)OC(=O)C(C)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description R-7128(Mericitabine) is a selective nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase.
Targets HCV          
IC50            

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

R-7128