LEI-401 |
| Catalog No.GC60982 |
Le LEI-401 est un inhibiteur NAPE-PLD (N-acylphosphatidyléthanolamine phospholipase D) premier de sa catégorie, sélectif et actif sur le SNC, avec une IC50 de 27 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2393840-15-6
Sample solution is provided at 25 µL, 10mM.
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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]
[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.
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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