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LEI-401
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LEI-401图片
CAS NO:2393840-15-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
LEI-401是一种首创的、选择性的、通过血脑屏障的NAPE-PLD(N-酰基磷酰乙醇胺磷脂酶D)抑制剂,IC50为27nM。LEI-401对小鼠情绪行为的调节。
Cas No.2393840-15-6
Canonical SMILESO=C(C1=NC(N2C[C@H](C3=CC=CC=C3)CCC2)=NC(N4C[C@@H](O)CC4)=C1)NCC5CC5
分子式C24H31N5O2
分子量421.54
溶解度DMSO: 100 mg/mL (237.23 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.