보세프레비르

보세프레비르 속성

보세프레비르 C화학적 특성, 용도, 생산

개요

In May 2011, the U.S. FDA approved boceprevir (SCH-503034), to be given in combination with peginterferon alfa plus ribavirin, for the treatment of patients with chronic hepatitis C genotype 1 viral infection. Boceprevir and telaprevir are the first hepatitis C virus (HCV) protease inhibitors to be approved for the treatment of HCV infection. Boceprevir is an inhibitor of HCV NS3-4A protease, an essential enzyme required by HCV for posttranslational processing of viral proteins into their mature forms. Boceprevir binds covalently, but reversibly, to the active site serine by addition of the hydroxyl group to the keto-amide functionality. Boceprevir inhibits HCV NS3-4A protease with a Ki of 14 nM. In cell culture, the EC₅₀ of boceprevir was 200 nM for an HCV replicon constructed from genotype 1b. Boceprevir was two-to threefold less potent against HCV replicon from genotypes 1a, 2, and 3. The potency of boceprevir decreased threefold in the presence of human serum. Boceprevir was discovered through a series of systematic truncations and modifications of a keto-amide undecapeptide lead molecule.
Boceprevir is synthesized by coupling of 3-amino-4- cyclobutyl-2-hydroxybutyramide or the related oxobutyramide with a cyclopropyl-pyrrolidine carboxylic acid intermediate. The pyrrolidine derivative can be prepared via cyclopropanation of a bicyclic lactam derivative or by conversion of 3,3-dimethylcyclopropane-1,2-dicarboxylic acid to the pyrrolidine in a multistep route. Boceprevir is a 1:1 mixture of diastereomers at the readily epimerizable position a to the keto group.

화학적 성질

Off-White to Pale Yellow Solid

용도

An NS3 serine protease inhibitor of hepatitis C virus, for the treatment of HCV infection. It is a COVID19-related research product.

정의

ChEBI: A synthetic tripeptide consisting of N-(tert-butylcarbamoyl)-3-methyl-L-valyl, a cyclopropyl-fused prolyl and 3-amino-4-cyclobutyl-2-oxobutanamide residues joined in sequence. Used for treatment of chronic h patitis C virus genotype 1 infection.

Clinical Use

Boceprevir is an oral inhibitor of HCV NS3/4A protease for the treatment of the chronic hepatitis C genotype infection. It is approved as combination therapy with Peg-IFN-alpha and ribavarin to treat adult patients with compensated liver diseasewhoare either treatment naive or who have experienced prior failed therapy with interferon and ribavarin. Boceprevir was initially discovered by Schering-Plough and developed and marketed by Merck & Co. since its acquisition of Schering-Plough in 2009. Several publications have highlighted the discovery of this drug, which evolved from a potent initial undecapeptide lead structure to boceprevir (VII) as a drug candidate with potent activity and desirable PK properties.

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보세프레비르 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Alpha Biopharmaceuticals Co., Ltd	+86-15542445688	sales@alabiochem.com	China	888	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21673	55
Shanghai Zheyan Biotech Co., Ltd.	18017610038	zheyansh@163.com	CHINA	3620	58
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29897	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
Chongqing Chemdad Co., Ltd	+86-023-6139-8061 +86-86-13650506873	sales@chemdad.com	China	39916	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49391	58
Nanjing Fred Technology Co., Ltd.	+86-02584696168 15380713688	Austin@fredchem.cn	CHINA	865	58
Shanxi Xuanran Import and Export Trade Co., Ltd.	+8617735180244	mike_yan@xuanranglobal.com	CHINA	4022	58
Dorne Chemical Technology co. LTD	+86-86-13583358881 +8618560316533	Ethan@dornechem.com	China	3146	58

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