940908-79-2 Usage
Biological Activity
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.
Check Digit Verification of cas no
The CAS Registry Mumber 940908-79-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,4,0,9,0 and 8 respectively; the second part has 2 digits, 7 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 940908-79:
(8*9)+(7*4)+(6*0)+(5*9)+(4*0)+(3*8)+(2*7)+(1*9)=192
192 % 10 = 2
So 940908-79-2 is a valid CAS Registry Number.
940908-79-2Relevant articles and documents
METHODS FOR TREATING HCV
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Paragraph 0353, (2013/10/22)
This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
PROCESS FOR THE PREPARATION OF 2-DEOXY-2-FLUORO-2-METHYL-D-RIBOFURANOSYL NUCLEOSIDE COMPOUNDS
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Paragraph 0057, (2014/01/07)
An improved process for the preparation of (2′R)-2′-deoxy-2′-fluoro-2′-methylcytidine derivatives of formula I wherein R1 is selected from C1-4-alkyl is described. The (2′R)-2′-deoxy-2′-fluoro-2′-methylcytidine derivatives of formula I have the potential to be useful as prodrugs for potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.
ANTIVIRAL NUCLEOSIDES
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Page/Page column 29-30, (2008/06/13)
Compounds having the formula I wherein R1 is as herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, and processes for making the compounds of formula I.
