Belnacasan (VX-765)

Catalog No.S2228

Belnacasan (VX-765) Chemical Structure

Molecular Weight(MW): 509

Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.

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3 Customer Reviews

  • BMMs were treated as above for 1 h. Cell lysates, as well as cell culture supernatants, were analyzed by western blot for cleavage of caspase-1. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) served as loading control.

    Mucosal Immunol, 2015, 10.1038/mi.2015.44. Belnacasan (VX-765) purchased from Selleck.

    (c,d) HMDMs and BMMs were treated as above for 1 h. Cell lysates, as well as cell culture supernatants, were analyzed by western blot for cleavage of caspase-1. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) served as loading control. Similar results were obtained in two independent experiments. Ctrl, control; DMSO, dimethyl sulfoxide.

    Mucosal Immunol, 2016, 9(1):124-36. Belnacasan (VX-765) purchased from Selleck.

  • (A) LPS-primed J774A.1 macrophages were treated with DCA (100 μM) in the presence or absence of caspase-1 inhibitor belnacasan (10 μM). IL-1β in supernatants was analyzed by ELISA.

    Front Immunol, 2016, 7:536.. Belnacasan (VX-765) purchased from Selleck.

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Biological Activity

Description Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.
Features A potent and selective inhibitor of interleukin-converting enzyme/caspase-1.
Targets
Caspase-4 [1]
(Cell-free assay)
Caspase-1 [1]
(Cell-free assay)
<0.6 nM(Ki) 0.8 nM(Ki)
In vitro

VX-765 is an orally absorbed prodrug of VRT-043198, which exhibits potent inhibition against ICE/caspase-1 and caspase-4 with Ki of 0.8 nM and less than 0.6 nM, respectively. And VRT-043198 also inhibits IL-1β release from both PBMCs and whole blood with IC50 of 0.67 μM and 1.9 μM, respectively. [1]

In vivo In collagen-induced arthritis mouse model, VX-765 (200 mg/kg) inhibits LPS-induced IL-1β production by about 60%, and results in a dose-dependent, statistically significant reduction in the inflammation scores and effective protection from joint changes. [1] In vivo, VX-765 blocks kindling epileptogenesis in rats by preventing IL-1β increase in forebrain astrocytes without significant effect on afterdischarge duration. [2] In the mouse model of acute seizures, VX-765 (50 mg/kg-200 mg/kg) produces the anticonvulsant effect by delaying the time to onset of the first seizure and decreasing the number of seizures as well as their total duration by average 50% and 64%. [3] In adult rats with genetic absence epilepsy (GAERS), VX-765, after the 3rd drug injection, significantly reduces the cumulative duration and number of spike-and-wave discharges (SWDs) by 55% on average by selectively blocking IL-1β biosynthesis. [4]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Collagen-induced arthritis mouse model.
  • Formulation: VX-765 is dissolved in 25% Cremophor EL.
  • Dosages: ≤200 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (196.46 mM)
Ethanol 100 mg/mL warmed (196.46 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 509
Formula

C24H33ClN4O6

CAS No. 273404-37-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01501383 Terminated Epilepsy Vertex Pharmaceuticals Incorporated December 2011 Phase 2
NCT01048255 Completed Partial Epilepsy Vertex Pharmaceuticals Incorporated January 2010 Phase 2
NCT00205465 Completed Psoriasis Vertex Pharmaceuticals Incorporated December 2004 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID