1446817-84-0

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.

Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.

Synthesis route for ABX-1431:

1) Cisar et al. (2018), Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders; J. Med. Chem., 61 9062