产品
编 号:F166094
分子式:C20H22F9N3O2
分子量:507.39
产品类型
结构图
CAS No: 1446817-84-0
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产品详情
生物活性:
Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
体内研究:
Elcubragistat (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.
体外研究:
Elcubragistat (ABX-1431) is a potent human MGLL inhibitor (IC50=0.014 μM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. Elcubragistat 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.