VX765 Inhibitor CAS No. 273404-37-8

Cat. No.	Name	Size	Price
KI2753	VX765	10 mg	$224
	VX765	25 mg	$470
	VX765	50 mg	$752
	VX765	100 mg	$1202
	VX765	200 mg	$1924
	VX765	500 mg	$3850

Chemical Characteristic

Product Name	VX765
Synonyms	VX-765,Belnacasan
CAS No.	273404-37-8
Molecular Weight	508.99
Formula	C₂₄H₃₃ClN₄O₆
Chemical Name	N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide
Smiles	C(=O)(C1N(CCC1)C(=O)[C@H](NC(=O)c1cc(c(cc1)N)Cl)C(C)(C)C)NC1[C@H](OC(=O)C1)OCC
Chemical Structure
Documents	HNMR CNMR HPLC LCMS

Biological activities

VX-765 is an orally-absorbed pro-drug of VRT-043198. VX-765 is a potent and selective inhibitor of interleukin converting enzyme (ICE)/caspase-1 sub-family caspases.^[1] VX-765 is currently under development for the treatment of inflammatory and autoimmune conditions.^[2] VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases. VRT-043198 potently inhibits ICE/caspase-1 and caspase-4 with Ki values of 0.8 nM and less than 0.6 nM, respectively. VRT-043198 inhibits IL-1β release from both PBMCs and whole blood with IC50s of 0.67 and 1.9 µM, respectively. VRT-043198 inhibits the release of IL-1β and IL-18 from human monocytes in vitro. In vivo in collagen-induced arthritis (CIA) mice, VX-765 induces a dose-dependent, significant reduction in the inflammation scores. Importantly, 100 mg/kg VX-765 is as efficacious as 5 mg/kg prednisolone.^[1]

Protocols

In vivo, VX-765 is prepared as a DMSO stock solution and diluted to appropriate concentrations in medium.^[2]

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, 321(2):509-516. [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, 175(4): 2630-2634.

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