VX 765
Chemical Name: N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide
Purity: ≥98%
Biological Activity
VX 765 is a high affinity and selective caspase-4 and caspase 1/ICE inhibitor (Ki 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Coptisine from coptis chinensis blocks NLRP3 inflammasome activation by inhibiting caspase-1.
Wu et al.
Pharmacol.Res., 2019;147:104348 -
IL-converting enzyme/caspase-1 inhibitor VX-765 blocks the hypersensitive response to an inflammatory stimulus in monocytes from familial cold autoinflammatory syndrome patients.
Stack et al.
J.Immunol., 2005;175:2630 -
Caspase-1 inhibitor exerts brain-protective effects against sepsis-associated encephalopathy and cognitive impairments in a mouse model of sepsis.
Xu et al.
Brain Behav.Immun., 2019;80:859 -
NLRP3 inflammasome activation promotes the development of allergic rhinitis via epithelium pyroptosis.
Yang et al.
Biochem.Biophys.Res.Commun., 2019;522:61 -
(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 inh
Wannamaker et al.
J.Pharmacol.Exp.Ther., 2007;321:509
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