Belnacasan

Belnacasan (VX-765) is an orally bioactive proagent of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE) /caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM[1][2].

Product Specifications

CAS Number

[273404-37-8]

Product Name Alternative

VX-765

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Caspase

Type

Reference compound

Related Pathways

Apoptosis

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/VX-765.html

Purity

99.99

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

ClC1=C(N)C=CC(C(N[C@@H](C(C)(C)C)C(N2[C@H](C(N[C@H]3CC(O[C@H]3OCC)=O)=O)CCC2)=O)=O)=C1

Molecular Formula

C24H33ClN4O6

Molecular Weight

509.00

Precautions

H302, H315, H319, H335

References & Citations

[1]Stack JH, et al. IL-converting enzyme/caspase-1 inhibitor VX-765 blocks the hypersensitive response to an inflammatory stimulus in monocytes from familial cold autoinflammatory syndrome patients. J Immunol. 2005 Aug 15;175 (4) :2630-4.|[2]Wannamaker W, et al. (S) -1- ((S) -2-{[1- (4-amino-3-chloro-phenyl) -methanoyl]-amino}-3,3-dimethyl-butanoyl) -pyrrolidine-2-carboxylic acid ((2R,3S) -2-ethoxy-5-oxo-tetrahydro-furan-3-yl) -amide (VX-765), an orally available selective interleukin (IL) -converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18. J Pharmacol Exp Ther. 2007 May;321 (2) :509-16.|[3]Ravizza T, et al. Inactivation of caspase-1 in rodent brain: a novel anticonvulsive strategy. Epilepsia. 2006 Jul;47 (7) :1160-8.