VX 765

Name: VX 765
Brand: Tocris Bioscience
SKU: 7143

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

Citations (8)

COA / SDS

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

100% Guarantee

Technical Data
Citations

Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

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

Alternative Names

Belnacasan

View all Caspase Inhibitors »

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

Molecular Weight

509.00

Formula

C₂₄H₃₃ClN₄O₆

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide

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.

Solubility

	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 509.00

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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

Background References

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 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