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Belnacasan

CAT: 0804-HY-13205-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13205-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
273404-37-8
Product Name Alternative
VX-765
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Caspase
Type
Reference compound
Related Pathways
Apoptosis
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/VX-765.html
Purity
99.99
Solubility
DMSO : 100 mg/mL (ultrasonic) |H2O : 1 mg/mL (ultrasonic; warming; heat to 60°C)
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
Molecular Formula
C24H33ClN4O6
Molecular Weight
509.00
Precautions
H302, H315, H319, H335
References & Citations
[1]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.|[2]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.|[3]Ravizza T, et al. Inactivation of caspase-1 in rodent brain: a novel anticonvulsive strategy. Epilepsia. 2006 Jul;47 (7) :1160-8.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Caspase 1