ABX-1431

ABX-1431CAS号: 1446817-84-0分子式: C20H22F9N3O2分子量: 507.39描述纯度储存/保存方法别名外观可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
Elcubragistat
外观
White solid
可溶性/溶解性
DMSO : 125 mg/mL (246.36 mM; Need ultrasonic)
生物活性
In vitro(体外研究)
ABX-1431 is a potent human MGLL inhibitor (IC50=0.014 µM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. ABX-1431 inhibits human PC3 cells with an IC50 of 0.0022 µM. In the cell-based assay, >100-fold selectivity for MGLL over ABHD6 (IC50=0.253 µM) and PLA2G7 (IC50=494 µM) is maintained.
In vivo(体内研究)
ABX-1431 inhibits MGLL activity in rodent brain (ED50=0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model.