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Submit ReviewVX 765
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)
Biological Activity for VX 765
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.
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 Data 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 | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets for VX 765
References for VX 765
References are publications that support the biological activity of the product.
Wu et al (2019) Coptisine from coptis chinensis blocks NLRP3 inflammasome activation by inhibiting caspase-1. Pharmacol.Res. 147 104348 PMID: 31336157
Wannamaker et al (2007) (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. 321 509 PMID: 17289835
Stack et al (2005) 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. 175 2630 PMID: 16081838
Xu et al (2019) Caspase-1 inhibitor exerts brain-protective effects against sepsis-associated encephalopathy and cognitive impairments in a mouse model of sepsis. Brain Behav.Immun. 80 859 PMID: 31145977
Yang et al (2019) NLRP3 inflammasome activation promotes the development of allergic rhinitis via epithelium pyroptosis. Biochem.Biophys.Res.Commun. 522 61 PMID: 31740004
If you know of a relevant reference for VX 765, please let us know.
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Keywords: VX 765, VX 765 supplier, VX765, high, affinity, selective, caspase4, caspase1, inhibitors, inhibits, anticonvulsant, anti-inflammatory, orally, bioavailable, IL-converting, enzyme, ICE, Belnacasan, Caspases, 7143, Tocris Bioscience
Citations for VX 765
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