ABX-1431

ABX-1431 is an inhibitor of monoacylglycerol lipase (MAGL, IC50s = 14 and 27 nM for human and rat enzyme, respectively). It is selective for MAGL over ABHD6 and PLA2G7 (IC50s = 2.7 and >10 µM, respectively), as well as a panel of 33 serine hydrolases and a panel of 95 enzymes, receptors, transporters, and ion channels at 10 µM. It is also selective for MAGL over the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, and CYP3A4/5 (IC50s = >50 µM). Ex vivo, ABX-1431 inhibits MAGL activity in mouse and rat brain (ED50s = 1.4 and 0.5 mg/kg, respectively). In vivo, ABX-1431 decreases brain levels of 2-arachidonoyl glycerol (2-AG, Cay-62160) in mice and rats and reduces formalin-induced paw-licking time in rats.Formal Name: 4-[[2-(1-pyrrolidinyl)-4-(trifluoromethyl)phenyl]methyl]-1-piperazinecarboxylic acid, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester. CAS Number: 1446817-84-0. Molecular Formula: C20H22F9N3O2. Formula Weight: 507.4. Purity: >98%. Formulation: (Request formulation change), A solution in methyl acetate. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml, Ethanol:PBS (pH 7.2) (1:10): 0.1 mg/ml. lambdamax: 264, 309 nm. SMILES: O=C(OC(C(F)(F)F)C(F)(F)F)N(CC1)CCN1CC2=CC=C(C(F)(F)F)C=C2N3CCCC3. InChi Code: 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. InChi Key: SQZJGTOZFRNWCX-UHFFFAOYSA-N.