Elcubragistat,1446817-84-0

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Elcubragistat

CAS No. : 1446817-84-0

MCE 国际站：Elcubragistat

产品活性：Elcubragistat (ABX-1431) 是一种高效，选择性和口服可用的 CNS-渗透性单酰基甘油脂肪酶 (MAGL) 抑制剂，IC₅₀ 为 14 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：MAGL

In Vitro: 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.

In Vivo: 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.

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