ABX-1431

SKU: orb1226260

Description

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL); displays 23-fold selectivity for MGLL versus ABHD6 and CES1c, as well as exquisite selectivity of against other members of the serine hydrolase class; 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.Pain Phase 1 Clinical(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.(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.

Key Properties

• CAS Number: 1446817-84-0
• MW: 507.401
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₂F₉N₃O₂
• SMILES: O=C(N1CCN(CC2=CC=C(C(F)(F)F)C=C2N3CCCC3)CC1)OC(C(F)(F)F)C(F)(F)F
• Target: MAGL
• Solubility: DMSO: 100 mg/mL, 197.08 mMWater: InsolubleEthanol: 10 mg/mL, 19.71 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ABX1431 | ABX 1431

Quick Database Links

Gene Symbol

MAGL