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Belnacasan

(Synonyms: VX-765)
172 Cited Publications
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Based on 172 publication(s) in Google Scholar

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.

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  • Reinheit: 99.99%
  • CAS. Nr.: 273404-37-8
  • Formel: C24H33ClN4O6
  • Molecular Weight:509.00
  • Speicherung:
    Powder   -20°C, 3 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Belnacasan Chemical Structure
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
  • Belnacasan Chemical Structure
    Belnacasan Chemical Structure
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
  • Experimental Validation Results for Belnacasan
CAS. Nr.: 273404-37-8
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  • Belnacasan Chemical Structure
    Belnacasan Chemical Structure
    1/16
  • 1/16

    Belnacasan purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2022 Aug;29(8):1486-1499. [Abstract]

    Customer Validation
     Flow cytometry of CD4 and CD8 T cells expressing caspase activity in the absence (Med) or presence of Q-VD-Oph (Q-VD) (10 μM) (Top). Inhibition of caspase activity (preventive effect) in the presence of IDN-6556 (10 μM), VX-765 (10 μM), Q-VD and MCC950. Percentages were calculated as follows: (Med-Inh/Med)*100. Each dot represents one individual (Middle). Flow cytometry of CD4 and CD8 T cells expressing annexin V in the absence (Med) or presence of Q-VD (Bottom).

  • 1/16

    Belnacasan purchased from MedChemExpress. Usage Cited in: J Leukoc Biol. 2019 Feb;105(2):401-410. [Abstract]

    Customer Validation
     PMA-differentiated CASP4/5-deficient THP-1 cells are primed with 100 ng/mL LPS for 4 h, and are then left uninfected or are infected with S. Typhimurium (MOI 25, log-phase), in the presence of 25 μM VX765 to suppress cell death and cellular release of the ASC speck.

  • 1/16

    Belnacasan purchased from MedChemExpress. Usage Cited in: Toxicology. 2018 Dec 1:410:26-40. [Abstract]

    Customer Validation
     HUVECs are primed with 1 μg/mL LPS for 2 h, and then pretreated with or without 5 μM VX-765 for 1 h; following by treatment with Acrolein (50 μM) for 24 h. Western blot is performed to determine the expression of cleaved caspase-1, IL-1β and IL-18.

  • 1/16

    Belnacasan purchased from MedChemExpress. Usage Cited in: Brain Behav Immun. 2017 Oct:65:99-110. [Abstract]

    Customer Validation
     VX765 treatment successfully inhibits the caspase 1 activity and reduces nuclear TDP-43 and cleaved caspase-3 protein levels in the hippocampus of BDE-47-treated mice.

  • 1/16

    Belnacasan purchased from MedChemExpress. Usage Cited in: Brain Behav Immun. 2016 Aug:56:175-86. [Abstract]

    Customer Validation
     The effects of NLRP3 inflammasome inhibitor VX-765 on NF-κB and CD11b levels in Sham and OVX groups. Sham operation or bilateral ovariectomy is performed and then the mice are subcutaneously administrated with the chemicals as indicated for four weeks. (A) p-p65 protein level with representative protein bands presented on top of histogram; (B) CD11b protein level with representative protein bands presented on top of histogram.

  • Belnacasan