VX-765

Catalog #

27779-1

$520 *

Size: 100 mg

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Description

VX-765, also known as Belnacasan, 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

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.

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