An inhibitor of MAGL
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ABX-1431

Item No. 26023

Technical Information
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
Purity
≥98%
Formulation
A 10 mg/ml solution in methyl acetate
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/mlEthanol:PBS (pH 7.2) (1:10): 0.1 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    ABX-1431 is an inhibitor of monoacylglycerol lipase (MAGL; IC50s = 14 and 27 nM for human and rat enzyme, respectively).1 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; Item No. 62160) in mice and rats and reduces formalin-induced paw-licking time in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cisar, J.S., Weber, O.D., Clapper, J.R., et alIdentification of ABX-1431, a selective inhibitor of monoacylglycerol lipase and clinical candidate for treatment of neurological disorders. J. Med. Chem. 61(20), 9062-9084 (2018).