Asunaprevir Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Enzyminhibitor

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Asunaprevir Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Shanghai Daken Advanced Materials Co.,Ltd	+86-371-66670886	info@dakenam.com	China	18754	58
Hubei XinRunde Chemical Co., Ltd.	+8615102730682	bruce@xrdchem.cn	CHINA	566	55
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29885	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	965	58
Nanjing Dolon Biotechnology Co.,Ltd.	18905173768	sales@dolonchem.com	CHINA	2972	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-6139-8061 +86-86-13650506873	sales@chemdad.com	China	39894	58
Hebei Binshare New Material Co. Ltd	+8618633865755	china01@hbbinshare.com	CHINA	955	58
Nanjing Fred Technology Co., Ltd.	+86-02584696168 15380713688	Austin@fredchem.cn	CHINA	865	58
Qiuxian Baitai New Material Co., LTD	+8618330912755	sale2@hbyalin.com	China	1658	58

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• (1R,2S)-N-[(1,1-Dimethylethoxy)carbonyl]-3-methyl-L-valyl-(4R)-4-[(7-chloro-4-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenylcyclopropanecarboxamide
• Asunaprevir
• BMS 650032
• Asunaprevir (BMS-650032)
• BMS 650032/Asunaprevir
• Asunaprevir API
• tert-butyl N-[(2S)-1-[(2S,4R)-4-(7-chloro-4-methoxyisoquinolin-1-yl)oxy-2-[[(1R,2S)-1-(cyclopropylsulfonylcarbamoyl)-2-ethenylcyclopropyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
• BMS-650032; BMS 650032; BMS650032
• CS-1413
• tert-Butyl ((2S)-1-((2S)-2-(((1R,2S)-1-amino-2-vinylcyclopropane-1-carbonyl)(cyclopropylsulfonyl)carbamoyl)-4-((7-chloro-4-methoxyisoquinolin-1-yl)oxy)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamate
• Asunaprevir,≥98%
• Cyclopropanecarboxamide, N-[(1,1-dimethylethoxy)carbonyl]-3-methyl-L-valyl-(4R)-4-[(7-chloro-4-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenyl-, (1R,2S)-
• Asunaprevir USP/EP/BP
• Asunaprevir (10mM in DMSO)
• 630420-16-5
• C35H46ClN5O9S
• API