Belnacasan (VX-765) 273404-37-8

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Molecular Weight:

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

Biological Activity

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.


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.


In
vivo, VX-765 blocks kindling epileptogenesis in rats by preventing IL-1β
increase in forebrain astrocytes without significant effect on
afterdischarge duration. 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%.


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.

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Product Categories : Proteases > Caspase Inhibitor