For research use only. Not for therapeutic Use.
Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
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[1].
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].
| Catalog Number | I019697 |
| CAS Number | 1446817-84-0 |
| Synonyms | 1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[2-pyrrolidin-1-yl-4-(trifluoromethyl)phenyl]methyl]piperazine-1-carboxylate |
| Molecular Formula | C20H22F9N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H22F9N3O2/c21-18(22,23)14-4-3-13(15(11-14)31-5-1-2-6-31)12-30-7-9-32(10-8-30)17(33)34-16(19(24,25)26)20(27,28)29/h3-4,11,16H,1-2,5-10,12H2 |
| InChIKey | SQZJGTOZFRNWCX-UHFFFAOYSA-N |
| SMILES | C1CCN(C1)C2=C(C=CC(=C2)C(F)(F)F)CN3CCN(CC3)C(=O)OC(C(F)(F)F)C(F)(F)F |
| Reference | [1]. Cisar JS, et al. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders. J Med Chem. 2018 Oct 25;61(20):9062-9084. |
