Elcubragistat (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MAGL) with IC50 of 14 nM (hMAGL).
Elcubragistat (ABX1431) displays 23-fold selectivity for MGLL versus ABHD6 and CES1c, as well as exquisite selectivity of against other members of the serine hydrolase class.
Elcubragistat (ABX1431) 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.
