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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.
CAS Number: 273404-37-8
Description: VX-765, also known as Belnacasan, is a novel Caspase-1 inhibitor being investigated for the treatment of epilepsy.
Solubility: Soluble in DMSO
Storage Stability: Store desiccated at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: Caspase1
Warnings: Protect from moisture.
Biosafety Level: Not applicable (BSL-1)
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.
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