VX 765

Name: VX 765
Brand: Tocris Bioscience
SKU: 7143

Tocris Bioscience, part of Bio-Techne | Catalog # 7143

Citations (3)

COA / SDS

High affinity and selective caspase-4 and caspase 1/ICE inhibitor; orally bioavailable

Key Product Details

Description:	High affinity and selective caspase-4 and caspase 1/ICE inhibitor; orally bioavailable
Alternative Names:	Belnacasan
Chemical Name:	N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide
Purity:	≥98% (HPLC)
Molecular Weight:	509

View Full Technical Details for VX 765

Technical Data
Citations

Biological Activity for VX 765

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.

Compound Libraries for VX 765

VX 765 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for VX 765

M. Wt	509
Formula	C₂₄H₃₃ClN₄O₆
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	273404-37-8
PubChem ID	11398092
InChi Key	SJDDOCKBXFJEJB-MOKWFATOSA-N
Smiles	CCO[C@@H]1OC(C[C@@H]1NC([C@@H]2CCCN2C([C@H](C(C)(C)C)NC(C3=CC(Cl)=C(C=C3)N)=O)=O)=O)=O

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.

Solubility for VX 765

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	50.9	100
	ethanol	50.9	100

Preparing Stock Solutions for VX 765

The following data is based on the product molecular weight 509.

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

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

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References for VX 765

References are publications that support the biological activity of the 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 inh 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