Name: TMC647055 Choline salt
Price: 464.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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].
    
    [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.
- Properties
  - CAS Number
    
    1204416-97-6
    
    Molecular Formula
    
    C37H53N5O8S
    
    Molecular Weight
    
    727.91
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥72.8 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

TMC647055 Choline salt

TMC647055 Choline salt

Background

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