(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

VX-765 shows anti-convulsant activity by inhibiting interlukin-1β biosynthesis.

Allgemeine Beschreibung

The cell-permeable prodrug of the caspase-1/4-selective inhibitor VRT-43198 (K_i in nM = <0.6/Caspase-4, 0.8/Caspase-1, 100/Caspase-8, 560/Caspase-6, 1,030/Caspase-9, 9,000/Granzyme B, 16,000/Caspase-7, 21,500/Caspase-3; IC₅₀ >100 μM against Cathepsin B & Trypsin). In addition to inhibiting LPS-induced IL-1β production in primary human PBMC cultures (IC₅₀ ~1 μM), VX-765 is also effective in preventing HIV infection-induced IL-1β production and pyroptosis of CD4 T cells in human lymphoid aggregate cultures (HLAC; CD4 population = 29.2% in non-infected control cultures, 8.3% vs. 30.2% in infected cultures with or without 5 μM VX-765). VX-765 is orally available in mice (Blood C_max = 0.78 μg/mL = 1.53 μM; T_max = 1.0 h; AUC_last = 2.06 μg · h/mL; 84 mg/kg, p.o.) and shown to display in vivo anti-inflammatory efficacy against LPS-induced plasma IL-1β production (ED_max = 100 mg/kg, p.o.), Oxazolone-induced delayed-type hypersensitivity (ED_max = 50 mg/kg, p.o.), collagen-induced arthritis (ED_max = 100 mg/kg, p.o.). When administered via intraperitoneal injection, VX-765 is also demonstrated to suppress the severity of seizure induction (ED_max = 50 mg/kg i.p.) among rats receiving kainic acid via intracerebroventricular injection.

Biochem/physiol Actions

Cell permeable: yes

(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Alpha Biopharmaceuticals Co., Ltd	+86-15542445688	sales@alabiochem.com	China	888	58
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9218	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32820	60
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	965	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28172	58
Changzhou PBpharmaceutical R&D Co.,Ltd	0519-83990708	info@pbpharm.com	CHINA	498	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Zhengzhou Alfa Chemical Co.,Ltd	+8618530059196	sale04@alfachem.cn	China	13486	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	31991	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10319	58

273404-37-8()Verwandte Suche:

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• (S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide
• Belnacasan (VX765)
• N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide
• L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-
• (S)-1-((S)-2-(4-Amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrah
• N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide VX 765
• VX-765(Belnacasan)
• CS-387
• VX 765; VX-765; VX765. BELNACASAN
• (2S)-1-[(2S)-2-[(4-amino-3-chlorophenyl)formamido]-3,3-dimethylbutanoyl]-N-[(2R,3S)-2-ethoxy-5-oxooxolan-3-yl]pyrrolidine-2-carboxamide
• BELNACASAN;VX-765;VX 765
• (S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide USP/EP/BP
• VX-765，VX 765
• Belnacasan
• Caspase-1-4 Inhibitor VX-765
• 273404-37-8
• C24H33ClN4O6
• Inhibitors
• API