Belnacasan(VX-765) , ≥98% , 273404-37-8

Synonym(s):
;Caspase-1/4 Inhibitor, VX-765 - CAS 273404-37-8 - Calbiochem

CAS NO.：273404-37-8

Empirical Formula: C24H33ClN4O6

Molecular Weight: 508.99

MDL number: MFCD11100350

PRODUCT Properties

• Boiling point: 779.0±60.0 °C(Predicted)
• Density: 1.32
• storage temp.: -20°C
• solubility: Soluble in DMSO (>25 mg/ml)
• pka: 12.60±0.40(Predicted)
• form: solid
• color: Off-white to white
• Stability: Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
• InChIKey: SJDDOCKBXFJEJB-MOKWFATOSA-N
• SMILES: C(N[C@H]1CC(=O)O[C@H]1OCC)(=O)[C@@H]1CCCN1C(=O)[C@H](C(C)(C)C)NC(=O)C1=CC=C(N)C(Cl)=C1

Description and Uses

Belnacasan (273404-37-8) is a prodrug of VRT-043198, a potent (Ki = 0.8 nM ICE/caspase-1; <0.6nM caspase-4) and selective inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases.1 VRT-043198 ICE/caspase-1 IC50 = 0.67 μM PBMCs, 1.0 μM whole blood. It inhibited the release of IL-1b and IL-18 from human monocytes in vitro and their production in vivo in models of inflammation. Belnacasan inhibited the activation and expression of the NLRP3 Inflammasome leading to moderation of depressive-like behaviors induced by chronic mild stress2 and prevention of glial pyroptosis in multiple sclerosis models3. It inhibited pyroptosis in vascular smooth muscle cells during atherogenesis suggesting a possible therapeutic effect in treating atherosclerotic disease.4 Belnacasan reduced acute seizures and drug resistant chronic epileptic activity in mice5 and provided neuroprotection in two rat models of temporal lobe epilepsy6. It also displays protective effects in models of stroke7and Alzheimer’s disease8.

VX-765 shows anti-convulsant activity by inhibiting interlukin-1β biosynthesis.

Safety

• Symbol(GHS): GHS07
• Signal word: warning
• Hazard statements: H315-H319-H335
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501
• WGK Germany: WGK 3
• Storage Class: 11 - Combustible Solids