LEI-401

LEI-401 is an inhibitor of N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD, IC50 = 0.86 µM in HEK293T cell membranes expressing the recombinant human enzyme). It is selective for NAPE-PLD over human cannabinoid (CB) receptor 1 (CB1), CB2, type IVE phospholipase A2, monoacylglycerol lipase (MAGL), and diacylglycerol lipase alpha (DAGLalpha), as well as mouse DAGLalpha, DAGLbeta, fatty acid amide hydrolase (FAAH), and alpha/beta-hydrolase domain-containing protein 6 (ABHD6), at 10 µM. LEI-401 (10 µM) reduces levels of a variety of N-acylethanolamines (NAEs), including N-palmitoylethanolamine (PEA), N-oleoylethanolamine (OEA), and N-arachidonoylethanolamine (AEA, Cay-90050), in Neuro2a cells. It impairs fear extinction in a cued fear conditioning test in mice when administered at a dose of 30 mg/kg.Formal Name: N-(cyclopropylmethyl)-6-[(3S)-3-hydroxy-1-pyrrolidinyl]-2-[(3S)-3-phenyl-1-piperidinyl]-4-pyrimidinecarboxamide. CAS Number: 2393840-15-6. Molecular Formula: C24H31N5O2. Formula Weight: 421.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml, DMSO: 5 mg/ml. lambdamax: 231 nm. SMILES: O=C(NCC1CC1)C2=CC(N3C[C@@H](O)CC3)=NC(N4C[C@H](C5=CC=CC=C5)CCC4)=N2. InChi Code: InChI=1S/C24H31N5O2/c30-20-10-12-28(16-20)22-13-21(23(31)25-14-17-8-9-17)26-24(27-22)29-11-4-7-19(15-29)18-5-2-1-3-6-18/h1-3,5-6,13,17,19-20,30H,4,7-12,14-16H2,(H,25,31)/t19-,20+/m1/s1. InChi Key: GFHJYPQZBBHOCC-UXHICEINSA-N.