보세프레비르

한글명:보세프레비르

카스 번호394730-60-0

상품명:Boceprevir

CBNumberCB32491465

분자식C27H45N5O5

포뮬러 무게519.68

MOL 파일394730-60-0.mol

동의어(한글)

보세프레비르

화학적 성질

녹는점	>107°C (dec.)
밀도	1.162
저장 조건	-20°C
용해도	DMSO에 용해됨(가온 시 최대 15mg/ml)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	12.82±0.40(Predicted)
색상	흰색 또는 황백색
안정성	제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.

위험 및 안전 성명

HS 번호

2933599590

유해 물질 데이터

394730-60-0(Hazardous Substances Data)

NFPA 704:

	0
2		0

그림문자(GHS)

보세프레비르 화학적 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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