VX765

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产品描述：

产品名称：VX765

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。

别名: Belnacasan; VX-765; VX 765

参考文献:

[1] Wannamaker W, et al. J Pharmacol Exp Ther. 2007, 321(2), 509-516.

[2] Ravizza T, et al. Neurobiol Dis. 2008, 31(3), 327-333.

[3] Maroso M, et al. Neurotherapeutics. 2011, 8(2), 304-315.

[4] Akin D, et al. Neurobiol Dis. 2011, 44(3), 259-269.

CAS号: 273404-37-8

靶点: Caspase-4 ,Caspase-1

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

外观: 白色粉末

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 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.

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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