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product name Belnacasan (VX-765)


Description: Belnacasan or VX-765, an orally bioactive prodrug of VRT-043198, is a potent and selective inhibitor of caspase-1 which belongs to the ICE/caspase-1 sub-family caspases.  VX-765 is usually metabolized to an active molecular VRT-043198. In cultures of peripheral blood mononuclear cells stimulated with bacterial products, VRT-043198 inhibited the release of Interleukin (IL)-1β and IL-18, but had no affect the secretion of other cytokines such as IL-α, TNFα, IL-6 and IL-8. This product is also used in other models to illustrate the function of Caspase-1. 

Reference: Cell Death Dis. 2012 Jul 5;3:e338.



Molecular Weight (MW)

508.99
Formula

C24H33ClN4O6 
CAS No.

273404-37-8
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 100 mg/mL warming (196.46 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 100 mg/mL warming (196.46 mM)
Solubility (In vivo)

 2% DMSO+30% PEG 300+ddH2O: 5 mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404735

General In a CIA mouse model, VX-765 significantly reduced the inflammation scores in a dose-dependent manner. In addition, 100 mg/kg VX-765 was as efficacious as 5 mg/kg Prednisolone.
Animal model Collagen-induced arthritis (CIA) mouse model
Formulation  VX-765 is dissolved in 25% Cremophor EL
Dosages 10, 25, 50 or 100 mg/kg
Administration  p.o.; b.i.d.; for 24 days.
Reference [1] Wannamaker W, et al. J Pharmacol Exp Ther. 2007, 321(2), 509-516.

Isavuconazole