全部商品分类
用小程序，查商品更便捷
产品介绍
产品介绍
产品信息
抗原名称
Caspase-4；Caspase-1
商品描述
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。
分子量
509.0
纯度
＞98%
可溶性
DMSO ：100 mg/mL warmed (196.46 mM)
Ethanol ：100 mg/mL warmed (196.46 mM)
Ethanol ：100 mg/mL warmed (196.46 mM)
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.
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.
背景
别名
Belnacasan；VX-765；VX 765
分子式
C24H33ClN4O6
CAS号
273404-37-8
制备和贮存
保存方式
store at -20℃ for one year（Powder）；
in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
参考图片
声明 ：本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。