R-7128NS5B inhibitor CAS# 940908-79-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 940908-79-2 | SDF | Download SDF |
PubChem ID | 16122663 | Appearance | Powder |
Formula | C18H26FN3O6 | M.Wt | 399.41 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | RG 7128; Mericitabine; PSI 6130 diisobutyrate | ||
Solubility | DMSO : 100 mg/mL (250.37 mM; Need ultrasonic) | ||
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 | ||
SMILES | CC(C)C(=O)OCC1C(C(C(O1)N2C=CC(=NC2=O)N)(C)F)OC(=O)C(C)C | ||
Standard InChIKey | MLESJYFEMSJZLZ-MAAOGQSESA-N | ||
Standard InChI | InChI=1S/C18H26FN3O6/c1-9(2)14(23)26-8-11-13(28-15(24)10(3)4)18(5,19)16(27-11)22-7-6-12(20)21-17(22)25/h6-7,9-11,13,16H,8H2,1-5H3,(H2,20,21,25)/t11-,13-,16-,18-/m1/s1 | ||
General tips | For 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | R-7128(Mericitabine) is a selective nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. | |||||
Targets | HCV |
R-7128 Dilution Calculator
R-7128 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.5037 mL | 12.5185 mL | 25.0369 mL | 50.0739 mL | 62.5923 mL |
5 mM | 0.5007 mL | 2.5037 mL | 5.0074 mL | 10.0148 mL | 12.5185 mL |
10 mM | 0.2504 mL | 1.2518 mL | 2.5037 mL | 5.0074 mL | 6.2592 mL |
50 mM | 0.0501 mL | 0.2504 mL | 0.5007 mL | 1.0015 mL | 1.2518 mL |
100 mM | 0.025 mL | 0.1252 mL | 0.2504 mL | 0.5007 mL | 0.6259 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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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.
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[Inhibitors of hepatitis C virus--current standards and status of investigations].[Pubmed:21473060]
Przegl Epidemiol. 2010;64(4):473-8.
The current standard of chronic hepatitis C therapy is the combined use of pegylated IFN-alpha 2a (PegIFN-alpha) and rybavirin (RBV). The new form of interferon, IFN-alpha 2b, was also introduced with no better results. Overall, the effectiveness of therapy with the use of the above scheme is not satisfactory. Thus the search for new therapeutic agents for hepatitis C is ongoing. These studies have the goal to find new preparations inhibiting the replication cycle of HCV. The new analogue of RBV, eg. tarybavirin was introduced, with lesser side effects, but the same effectiveness. The activity of new agents relies upon the inhibition of the most important enzymes of the HCV replication cycle: RNA polymerase, protease and helicase. Polymerase NS5 inhibitors are divided into nucleoside (R-7128) and nonnucleoside (ANA-598, GS 9190, VCH-759, VX-222). The intensive studies on the R-7128 analogue are ongoing. The effects of action of particular compounds in the I and II studies were summarized. The promised prodrug is nonnucleoside polymerase inhibitor, ANA-598 which when administrated to patients, gave 75% SVR. The combined administration of the newly described agents is the basis of specifically targeted antiviral therapies for HCV (STAT-C). These therapies allow to achieve better effectiveness of treatment, its shortening, the diminishment and limitation of side effects.