Asunaprevir

한글명:Asunaprevir

카스 번호630420-16-5

상품명:Asunaprevir

CBNumberCB92614356

분자식C35H46ClN5O9S

포뮬러 무게748.29

MOL 파일630420-16-5.mol

화학적 성질

녹는점	149-150oC
밀도	1.37
저장 조건	-20°C Freezer, Under inert atmosphere
용해도	DMSO(약간 용해됨), 메탄올(약간 용해됨, 가열)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	4.49±0.40(Predicted)
색상	흰색에서 황백색까지

그림문자(GHS)

Asunaprevir 화학적 특성, 용도, 생산

개요
Sold under the trade name Sunvepra®, asunaprevir received approval in Japan as part of a combination treatment for the hepatitis C virus (HCV). Working in concert with daclatasvir (IX) (vide infra), asunaprevir is a unique treatment for HCV, as it is free from both interferon and ribavirin and is administered orally. This direct-acting anti-viral, which was developed by Bristol–Myers Squibb (BMS), works as an NS3/4A protease inhibitor, representing a valuable treatment option for patient populations who are unable to receive, or do not respond to, the standard course of treatment—peginterferon/ribavirin.
효소 저해제
This highly selective HCV antiviral (FW = 748.29 g/mol; CAS 630420-16- 5; Symbol: ASV), also named BMS-650032, targets NS3 protease, a serine proteinase required for Hepatitis C Virus (HCV) polyprotein processing, showing good antiviral activity against replicons based on HCV Genotype 1a (EC50 = 4 nM), Genotype 1b (EC50 = 1.2 nM), Genotype 4 (EC50 = 1.8 nM), Genotype 5 (EC50 = 1.7 nM), and Genotype 6 (EC50 = 0.9 nM). It is far less effective against Genotype 2 (EC50 = 67 nM) and Genotype 3 (EC50 = >1100 nM). Asunaprevir is a peptidomimetic that occupies the active site, inhibiting the HCV NS3/4A serine protease, with little or no action against related viruses. The average Ki for ASV is approximately 0.4 nM and 0.2 nM for Genotype 1a and Genotype 1b, respectively. Its acylsulfonamide moeity interacts noncovalently with the NS3 protease – unlike telaprevir’s α-ketoamide moiety, which is linked covalently to NS3/4A’s catalytic serine and reverses slowly over time. ASV exhibits an excellent selectivity index (>40,000x) against all serine/cysteine proteases evaluated, including human leukocyte elastase, porcine pancreatic elastase, and three members of the chymotrypsin family. Although ASV shows a low barrier to resistance, it can be combined with daclatasvir to achieve a very high rate of viral eradication in both na?ve and treatment-experienced patients, showing a sustained virological response rate of 80%-90%.

Asunaprevir 준비 용품 및 원자재

Asunaprevir 공급 업체

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