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

(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide Struktur
273404-37-8
CAS-Nr.
273404-37-8
Englisch Name:
(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide
Synonyma:
Belnacasan;CS-387;VX-765,VX 765;Belnacasan (VX765);VX-765(Belnacasan);BELNACASAN;VX-765;VX 765;Caspase-1-4 Inhibitor VX-765;VX 765; VX-765; VX765. BELNACASAN;(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
CBNumber:
CB72513725
Summenformel:
C24H33ClN4O6
Molgewicht:
508.99
MOL-Datei:
273404-37-8.mol

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

Siedepunkt:
779.0±60.0 °C(Predicted)
Dichte
1.32
storage temp. 
-20°C
Löslichkeit
Soluble in DMSO (>25 mg/ml)
Aggregatzustand
solid
pka
12.60±0.40(Predicted)
Farbe
Off-white to white
Stabilität:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

(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 (Ki 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 Cmax = 0.78 μg/mL = 1.53 μM; Tmax = 1.0 h; AUClast = 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 (EDmax = 100 mg/kg, p.o.), Oxazolone-induced delayed-type hypersensitivity (EDmax = 50 mg/kg, p.o.), collagen-induced arthritis (EDmax = 100 mg/kg, p.o.). When administered via intraperitoneal injection, VX-765 is also demonstrated to suppress the severity of seizure induction (EDmax = 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 Händler.

Global( 129)Lieferanten
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 9337 55
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32760 60
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 967 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28180 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
Hubei Ipure Biology Co., Ltd
+8613367258412
ada@ipurechemical.com China 10326 58
HONG KONG IPURE BIOLOGY CO.,LIMITED
86 18062405514 18062405514
ada@ipurechemical.com CHINA 3465 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 25655 58

273404-37-8()Verwandte Suche:


  • (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
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