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ABX-1431

Chemical Structure : ABX-1431

CAS No.: 1446817-84-0

ABX-1431 (ABX1431;Elcubragistat)

Catalog No.: PC-35522Not For Human Use, Lab Use Only.

Elcubragistat (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

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Biological Activity

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

Physicochemical Properties

M.Wt 507.401
Formula C20H22F9N3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1,1,1,3,3,3-hexafluoropropan-2-yl-4-[[2-(pyrrolidin-1-yl)-4-(trifluoromethyl)phenyl]methyl]piperazine-1-carboxylate

References

1. Cisar JS, et al. J Med Chem. 2018 Aug 1. doi: 10.1021/acs.jmedchem.8b00951.

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