Elcubragistat


CAS No. : 1446817-84-0

(Synonyms: ABX-1431)

1446817-84-0
Price and Availability of CAS No. : 1446817-84-0
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5mg $53 In-stock
10mg $83 In-stock
25mg $165 In-stock
50mg $275 In-stock
100mg $495 In-stock
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Cat. No. : HY-117632
M.Wt: 507.39
Formula: C20H22F9N3O2
Purity: >98 %
Solubility: DMSO : 250 mg/mL (ultrasonic)
Introduction of 1446817-84-0 :

Elcubragistat (ABX-1431) is a highly effective, selective, orally active, and blood-brain barrier-permeable monoacylglycerol lipase (MAGL) inhibitor, with an IC50 value of 14 nM[1]. IC50 & Target:IC50: 14 nM (human MGLL)[1] In Vitro: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]. 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].

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