Description
ABX-1431 (1446817-84-0) is a potent (IC50 = 14 nM in vitro, 2.2 nM in human PC3 cells) and very selective (>100-fold over hABHD6, >200-fold over hPLA2G7) inhibitor of monoacylglycerol lipase (MAGL).1 Active in a rat formalin pain test at 3mg/kg. Orally bioavailable and CNS penetrant.
Uses
Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
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[1].
References
[1] JUSTIN S. CISAR. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders[J]. Journal of Medicinal Chemistry, 2018, 61 20: 9062-9084. DOI:
10.1021/acs.jmedchem.8b00951
