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产品描述:

产品名称:VX765

靶点: Caspase-4;Caspase-1

CAS号: 273404-37-8

描述:

Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂,无细胞试验中Ki为0.8 nM。

中文别名: Belnacasan;VX-765;VX 765

外观: White powder

In vitro(体外研究): 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.

分子式: C24H33ClN4O6

In vivo(体内研究): 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 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.

分子量: 509.0

纯度: >98%

储存/保存方法: store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

可溶性/溶解性: DMSO :100 mg/mL warmed (196.46 mM)
Ethanol :100 mg/mL warmed (196.46 mM)

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