Telaprevir
- CAS No.
- 402957-28-2
- Chemical Name:
- Telaprevir
- Synonyms
- Incivek;CS-61;VX-950;MP-424;CS-1855;LY-570310;elaprevir;Telaprevir;tellaprevir;Telaprevir-d4
- CBNumber:
- CB41519837
- Molecular Formula:
- C36H53N7O6
- Molecular Weight:
- 679.85
- MOL File:
- 402957-28-2.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/6/30 15:45:59
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS08 |
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Signal word | Warning | |||||||||
Hazard statements | H361fd | |||||||||
Precautionary statements | P201-P202-P280-P308+P313-P405-P501 | |||||||||
Safety Statements | 24/25 | |||||||||
HS Code | 29339900 | |||||||||
NFPA 704 |
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Telaprevir price More Price(2)
Telaprevir Chemical Properties,Uses,Production
Description
The hepatitis C virus (HCV) protease inhibitor telaprevir (VX-950, MP- 424,LY-570310) was approved by the U.S. FDA in May 2011 for the treatment of genotype 1 chronic HCV infection in adult patients in combination with peginterferon alfa and ribavirin (PR). Telaprevir and boceprevir (vide supra) are the first two HCV protease inhibitors to be approved for treatment of HCV infection. Telaprevir is a HCV NS3-4A protease inhibitor that exerts its antiviral effect by blocking the release of nonstructural viral proteins from a polyprotein precursor. Telaprevir is a potent inhibitor of the protease (IC50=10 nM) and is active in cell culture (HCV 1b replicon assay, EC50=354 nM). Telaprevir was identified from efforts to truncate a decamer peptide inhibitor derived from the natural substrate NS5A-5B and was guided by structure-based design. The ketoamide group of telaprevir forms a covalent, reversible bond with the active site serine hydroxyl of the protease and compensates for the loss of affinity resulting from truncation of the peptide. Despite the presence of the reactive keto-amide group, telaprevir is >500-fold less potent against other serine proteases. Synthesis of the key octahydrocyclopenta[c]pyrrole-1-carboxylic acid fragment of telaprevir is achieved by a-deprotonation of Boc-protected 3-azabicyclo[3.3.0]nonane followed by reaction with CO2 and resolution of the racemic acid. Alternatively, deprotonation is carried out in the presence of a chiral amine to give the enantiomerically enriched acid.
Chemical Properties
Telaprevir is White Solid
Uses
Telaprevir is a peptidomimetic inhibitor of hepatitis C virus protease.
Definition
ChEBI: An oligopeptide consisting of N-(pyrazin-2-ylcarbonyl)cyclohexylalanyl, 3-methylvalyl, octahydrocyclopenta[c]pyrrole-1-carboxy, and 3-amino-N-cyclopropyl-2-oxohexanamide residues joined in sequence. Used f r treatment of chronic hepatitis C virus genotype 1 infection.
Clinical Use
Telaprevir is a potent peptide mimetic inhibitor of Hepatitis C virus (HCV) and works via covalent reversible binding to the NSV-3A protease enzyme. Telaprevir was discovered and developed by Vertex pharmaceuticals. The drug is marketed as an oral treatment for HCV infection in combination with Peg interferon and ribavarin for patients who are refractory to the initial standard therapy. The initial SAR studies and the discovery of teleprevir have been published. In addition, a full review of the discovery process that led to the development of telaprevir, including several iterations of the syntheses of teleprevir leading to the process route, has been reported.
Telaprevir Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
BDR Pharmaceuticals International Pvt Ltd | +91-2240560560 +91-7718884418 | Maharashtra, India | 206 | 58 | Inquiry |
GLENMARK LIFE SCIENCES LTD | +91 22 4018 9999 | New Delhi, India | 103 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
Chiral Biosciences Limited | 09441920381 | Mallapur, India | 41 | 58 | Inquiry |
Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
Chiral BioSciences Ltd | 91-9133330369 | Mallapur, India | 10 | 58 | Inquiry |
BDR Pharmaceuticals International Pvt., Ltd. | 91-22-40560560 | Maharashtra, India | 91 | 58 | Inquiry |
Archerchem Healthcare Pvt., Ltd. (part of Archerchem Group) | 91-22-42361111 | Maharashtra, India | 147 | 58 | Inquiry |
Global Chem Asia Pacific | 91-9849161572 | Hyderabad, India | 255 | 58 | Inquiry |