LEI-401_product_DataBase

Bioactivity

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].

Invitro

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].

In Vivo

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:

Name

LEI-401

CAS

2393840-15-6

Formula

C24H31N5O2

Molar Mass

421.54

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

LEI-401

CAS: 2393840-15-6 F: C24H31N5O2 W: 421.54