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TMC647055
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TMC647055图片
CAS NO:1204416-97-6
规格:98%
分子量:606.73
包装与价格:
包装价格(元)
5mg电议
25mg电议
500mg电议
1g电议

产品介绍
inhibitor of the hepatitis C virus NS5B polymerase
CAS:1204416-97-6
分子式:C32H38N4O6S
分子量:606.73
纯度:98%
存储:Store at -20°C

Background:

TMC647055 is a potent and selective non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase with EC50 value of 82 nM [1].


Hepatitis C virus (HCV) NS5B polymerase is a RNA-dependant RNA-polymerase that is responsible for viral replication and plays an important role in HCV life cycle. HCV is a major cause of chronic liver disease and acute hepatitis, ultimately leading to liver failure, cirrhosis and hepatocellular carcinoma [1].


TMC647055 is a selective and cell-permeating HCV NS5B inhibitor. In RNA polymerase primer-dependent transcription assay, TMC647055 inhibited HCV NS5B polymerase with IC50 value of 34 nM. In the Huh7-Luc cell line, TMC647055 inhibited the replication of genotype 1b replicon with EC50 values of 77 and 139 nM measured with luciferase readout and qRT-PCR readout, respectively. TMC647055 exhibited high-affinity interaction with NS5B across all genotypes (except for genotype 2b) with median KD value< 35 nM. In Huh7-Luc replicon cells, TMC647055 (750 nM) reduced 30 cell colonies formation. Also, TMC647055 (1.5 μM and 3.75 μM) reduced HCV replicon RNA [2] [3].


参考文献:
[1].  Vendeville S, Lin TI, Hu L, et al. Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055. Bioorg Med Chem Lett, 2012, 22(13): 4437-4443.
[2].  Devogelaere B, Berke JM, Vijgen L, et al. TMC647055, a potent nonnucleoside hepatitis C virus NS5B polymerase inhibitor with cross-genotypic coverage. Antimicrob Agents Chemother, 2012, 56(9): 4676-4684.
[3].  Cummings MD, Lin TI, Hu L, et al. Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase. J Med Chem, 2014, 57(5): 1880-1892.