VX-765
Catalog #
27779-2
$190
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Description
VX-765 is a novel Caspase-1 inhibitor being investigated for the treatment of epilepsy.
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Synonyms
VX-765; VX765; Belnacasan; (2S)-1-[(2S)-2-[(4-amino-3-chlorobenzoyl)amino]-3,3-dimethylbutanoyl]-N-[(2R,3S)-2-ethoxy-5-oxooxolan-3-yl]pyrrolidine-2-carboxamide
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥96%
Target(s)
Caspase1
Formula
C24H33ClN4O6
MW
508.99 Da
Solubility
Insoluble in H2O; ≥313 mg/mL in DMSO; ≥50.5 mg/mL in EtOH with ultrasonic
CAS Registry #
273404-37-8
Background
VX-765 is an orally-absorbed pro-drug of VRT-043198, a potent and selective inhibitor of ICE/caspase-1 sub-family caspases. VRT-043198 exhibits 100-10,000-fold selectivity against other caspase-3 and -6-9. In cultures of peripheral blood mononuclear cells and whole blood from healthy subjects stimulated with bacterial products, VRT-043198 inhibited the release of Interleukin (IL)-1beta and IL-18, but had little effect on the release of several other cytokines, including IL-1alpha, tumor necrosis factor-alpha, IL-6 and IL-8. VX-765 has been shown to inhibit acute seizures in preclinical models of acute epilepsy and has shown activity in preclinical models of chronic epilepsy that do not respond to standard anti-epileptic drugs.
References
1. Boxer MB, et al. ChemMedChem. 2010 May 3;5(5):730-8.
2. Wannamaker W, et al. J Pharmacol Exp Ther. 2007 May;321(2):509-16.
2. Wannamaker W, et al. J Pharmacol Exp Ther. 2007 May;321(2):509-16.