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Belnacasan
$55 – $540
Products Details
Product Description
– Belnacasan (VX-765) is an orally bioactive proagent of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM[1][2].
Web ID
– HY-13205
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C24H33ClN4O6
References
– [1]Wannamaker W, et al. (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 May;321(2):509-16.|[2]Stack JH, et al. 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 Aug 15;175(4):2630-4.|[3]Ravizza T, et al. Inactivation of caspase-1 in rodent brain: a novel anticonvulsive strategy. Epilepsia. 2006 Jul;47(7):1160-8.
CAS Number
– 273404-37-8
Molecular Weight
– 509.00
Compound Purity
– 99.99
SMILES
– ClC1=C(N)C=CC(C(N[C@@H](C(C)(C)C)C(N2[C@H](C(N[C@H]3CC(O[C@H]3OCC)=O)=O)CCC2)=O)=O)=C1
Clinical Information
– Phase 2
Research Area
– Inflammation/Immunology
Solubility
– DMSO : 100 mg/mL (ultrasonic)|H2O : 1 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Caspase
Isoform
– Caspase 1
Pathway
– Apoptosis
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
