VX 765

Key Product Details

Product Description

VX 765 is a high affinity and selective caspase-4 and caspase 1/ICE inhibitor (K_i of <0.6 and 0.8 nM, respectively). Prodrug of VRT-043198. Inhibits LPS-induced IL-1β production ~ 60% in collagen-induced arthritis mouse model. Exhibits anticonvulsant effects in mouse model of acute seizures. Anti-inflammatory. Orally bioavailable.

Product Specifications for VX 765

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for VX 765

The following data is based on the product molecular weight 509.00.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.96 mL	9.82 mL	19.65 mL
5 mM	0.39 mL	1.96 mL	3.93 mL
10 mM	0.20 mL	0.98 mL	1.96 mL
50 mM	0.04 mL	0.20 mL	0.39 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 7 publications citing the usage of this product.

• Yang NLRP3 inflammasome activation promotes the development of allergic rhinitis via epithelium pyroptosis. Biochem.Biophys.Res.Commun. 2019 PMID: 31740004
• Xu Caspase-1 inhibitor exerts brain-protective effects against sepsis-associated encephalopathy and cognitive impairments in a mouse model of sepsis. Brain Behav.Immun. 2019 PMID: 31145977
• Wannamaker (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 PMID: 17289835
• Stack 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 PMID: 16081838
• Wu Coptisine from coptis chinensis blocks NLRP3 inflammasome activation by inhibiting caspase-1. Pharmacol.Res. 2019 PMID: 31336157

Product Documents for VX 765