Welcome to LookChem.com Sign In|Join Free

CAS

  • or

1204416-97-6

Post Buying Request

1204416-97-6 Suppliers

Recommended suppliersmore

  • Product
  • FOB Price
  • Min.Order
  • Supply Ability
  • Supplier
  • Contact Supplier

1204416-97-6 Usage

Biological Activity

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].

references

[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.

Check Digit Verification of cas no

The CAS Registry Mumber 1204416-97-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,0,4,4,1 and 6 respectively; the second part has 2 digits, 9 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1204416-97:
(9*1)+(8*2)+(7*0)+(6*4)+(5*4)+(4*1)+(3*6)+(2*9)+(1*7)=116
116 % 10 = 6
So 1204416-97-6 is a valid CAS Registry Number.

1204416-97-6SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name 2,19-methano-3,7:4,1-dimetheno-1H,11H-14,10,2,9,11,17-benzoxathiatetraazacyclodocosine-8,18(9H,15H)-dione

1.2 Other means of identification

Product number -
Other names UNII-11BD024G7J

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1204416-97-6 SDS

1204416-97-6Relevant articles and documents

Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase

Cummings, Maxwell D.,Lin, Tse-I,Hu, Lili,Tahri, Abdellah,McGowan, David,Amssoms, Katie,Last, Stefaan,Devogelaere, Benoit,Rouan, Marie-Claude,Vijgen, Leen,Berke, Jan Martin,Dehertogh, Pascale,Fransen, Els,Cleiren, Erna,Van Der Helm, Liesbet,Fanning, Gregory,Nyanguile, Origène,Simmen, Kenny,Van Remoortere, Pieter,Raboisson, Pierre,Vendeville, Sandrine

, p. 1880 - 1892 (2014/04/03)

Structure-based macrocyclization of a 6-carboxylic acid indole chemotype has yielded potent and selective finger-loop inhibitors of the hepatitis C virus (HCV) NS5B polymerase. Lead optimization in conjunction with in vivo evaluation in rats identified several compounds showing (i) nanomolar potency in HCV replicon cells, (ii) limited toxicity and off-target activities, and (iii) encouraging preclinical pharmacokinetic profiles characterized by high liver distribution. This effort culminated in the identification of TMC647055 (10a), a nonzwitterionic 17-membered-ring macrocycle characterized by high affinity, long polymerase residence time, and broad genotypic coverage. In vitro results of the combination of 10a with the HCV protease inhibitor TMC435 (simeprevir) supported an evaluation of this combination in patients with regard to virus suppression and resistance emergence. In a phase 1b trial with HCV genotype 1-infected patients, 10a was considered to be safe and well-tolerated and demonstrated potent antiviral activity, which was further enhanced in a combination study with TMC435.

Structure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic properties

Cummings, Maxwell D.,Lin, Tse-I,Hu, Lili,Tahri, Abdellah,McGowan, David,Amssoms, Katie,Last, Stefaan,Devogelaere, Benoit,Rouan, Marie-Claude,Vijgen, Leen,Berke, Jan Martin,Dehertogh, Pascale,Fransen, Els,Cleiren, Erna,Van Der Helm, Liesbet,Fanning, Gregory,Van Emelen, Kristof,Nyanguile, Origene,Simmen, Kenny,Raboisson, Pierre,Vendeville, Sandrine

, p. 4637 - 4640 (2012/07/03)

The concept of drug-likeness distills the physicochemical properties of small-molecule drugs to a set of rules. Macrocyclic drugs are known to break these rules. A structure-based macrocyclization strategy was applied to design new hepatitis C virus NS5B inhibitors with improved pharmacokinetic properties, exemplifying a rational strategy for overcoming the confines of standard drug-like chemical space . Copyright

Post a RFQ

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

1

What can I do for you?
Get Best Price

Get Best Price for 1204416-97-6