| Identification | Back Directory | [Name]
4-Pyrimidinecarboxamide, N-(cyclopropylmethyl)-6-[(3S)-3-hydroxy-1-pyrrolidinyl]-2-[(3S)-3-phenyl-1-piperidinyl]- | [CAS]
2393840-15-6 | [Synonyms]
LEI-401
4-Pyrimidinecarboxamide, N-(cyclopropylmethyl)-6-[(3S)-3-hydroxy-1-pyrrolidinyl]-2-[(3S)-3-phenyl-1-piperidinyl]- | [Molecular Formula]
C24H31N5O2 | [MDL Number]
MFCD32857148 | [MOL File]
2393840-15-6.mol | [Molecular Weight]
421.54 |
| Hazard Information | Back Directory | [Biological Activity]
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice[1].
LEI-401 reduced a broad range of NAEs including anandamide in neuronal cells in a NAPE-PLD-dependent manner. LEI-401 (0.04-20 μM; 30 minutes) dose-dependently reduces the labeling of NAPE-PLD with an IC50 of 0.86 μM in hNAPE-PLD-transfected HEK293T cells. LEI-401 reduces NAE levels in Neuro-2a cells, but not in NAPE-PLD KO cells[1].
LEI-401 (30 mg/kg; i.p.) diminishes fear extinction in mice[1].LEI-401 also activates HPA axis signaling[1].LEI-401 (10 mg/kg; p.o.) treatment shows the t1/2, Cmax, tmax, AUClast, and F values of 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively[1].LEI-401 (30 mg/kg; i.p.) treatment show the Cmax, tmax, AUClast, and F values of 10300 ng/mL, 1 hour, 38600 h*ng/mL, and 48%, respectively[1]. Animal Model: Male 7-12-week-old C57BL/6J mice[1] | [storage]
Store at -20°C | [References]
[1]. Mock ED, et al. Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice. Nat Chem Biol. 2020;16(6):667-675. |
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