テラプレビル-D4

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

テラプレビル-D4 価格

テラプレビル-D4 化学特性,用途語,生産方法

• 効能

  抗ウイルス薬, プロテアーゼ阻害薬

• 説明

  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.

• 化学的特性

  Telaprevir is White Solid

• 使用

  Telaprevir is a peptidomimetic inhibitor of hepatitis C virus protease.

• 定義

  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.

• 臨床応用

  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.

テラプレビル-D4 上流と下流の製品情報

テラプレビル-D4 生産企業

Global(286)Suppliers

テラプレビル-D4 スペクトルデータ(MS)

402957-28-2, テラプレビル-D4 キーワード