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    Belnacasan (VX765)
    Belnacasan (VX765)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0024
    CAS #: 273404-37-8Purity ≥98%

    Description: Belnacasan (also known as VX-765) is a novel, potent, selective and orally bioactive prodrug of VRT-043198 which is a potent and selective inhibitor of caspase-1 with Ki values of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18. Caspase-1 belongs to the IL-converting enzyme (ICE)/caspase-1 sub-family caspases. VX-765 is usually metabolized to an active molecular VRT-043198. In cultures of peripheral blood mononuclear cells stimulated with bacterial products, VRT-043198 inhibited the release of Interleukin (IL)-1β and IL-18, but had no affect the secretion of other cytokines such as IL-α, TNFα, IL-6 and IL-8. This product is also used in other models to illustrate the function of Caspase-1. 

    References: 

    1. Cell Death Dis. 2012 Jul 5;3:e338;

    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. 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.


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    Molecular Weight (MW)508.99
    FormulaC24H33ClN4O6 
    CAS No.273404-37-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL warming (196.46 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: 100 mg/mL warming (196.46 mM)
    Other infoSolubility (In vivo): 2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
    Synonym: VX 765, VX765, VX-765, Belnacasan

    Chemical Name: (S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide

    SMILES Code: O=C([[email protected]]1N(C([[email protected]@H](NC(C2=CC=C(N)C(Cl)=C2)=O)C(C)(C)C)=O)CCC1)N[[email protected]@H](C3)[[email protected]](OCC)OC3=O


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    GeneralIn a CIA mouse model, VX-765 significantly reduced the inflammation scores in a dose-dependent manner. In addition, 100 mg/kg VX-765 was as efficacious as 5 mg/kg Prednisolone.
    Animal modelCollagen-induced arthritis (CIA) mouse model
    Formulation VX-765 is dissolved in 25% Cremophor EL
    Dosages10, 25, 50 or 100 mg/kg
    Administration p.o.; b.i.d.; for 24 days.
    References[1] Wannamaker W, et al. J Pharmacol Exp Ther. 2007, 321(2), 509-516.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Belnacasan (VX-765)

    Dose response of VX-765 in LPS-induced IL-1β production in vivo. Wannamaker W, et al. J Pharmacol Exp Ther. 2007 May;321(2):509-16.

    Belnacasan (VX-765)

    Effects of VX-765 on ear swelling induced by oxazolone.J Pharmacol Exp Ther. 2007 May;321(2):509-16.
     

    Belnacasan (VX-765)

    Effects of VX-765 on production of inflammatory mediators in biopsy samples from oxazolone-challenged mouse ears (n = 6/group). J Pharmacol Exp Ther. 2007 May;321(2):509-16.

    Belnacasan (VX-765)

    Effects of VX-765 on forepaw inflammation in the mouse CIA model administered in either the prophylactic (A) or therapeutic (B) regimen. J Pharmacol Exp Ther. 2007 May;321(2):509-16.




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