텔라프리비르

텔라프리비르 속성

텔라프리비르 C화학적 특성, 용도, 생산

개요

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.

화학적 성질

Telaprevir is White Solid

용도

Telaprevir is a peptidomimetic inhibitor of hepatitis C virus protease.

정의

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.

텔라프리비르 준비 용품 및 원자재

원자재

준비 용품

텔라프리비르 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Alpha Biopharmaceuticals Co., Ltd	+86-411-39042497 +8613921981412	sales@alphabiopharm.com	China	886	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1811	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21687	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9340	55
Shanghai Yingrui Biopharma Co., Ltd.	+86-21-33585366 - 03@	sales03@shyrchem.com	CHINA	738	60
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32715	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58

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