ABX-1431 (Synonyms: ABX-1431) |
| Catalog No.GC19412 |
ABX-1431 est un inhibiteur de la monoacylglycérol lipase (MAGL) pénétrant dans le SNC très puissant, sélectif et disponible par voie orale avec une IC50 de 14 nM.
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Cas No.: 1446817-84-0
Sample solution is provided at 25 µL, 10mM.
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ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
ABX-1431 is a potent human MGLL inhibitor (IC50=0.014 µM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. ABX-1431 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].
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].
[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.
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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