1. Metabolic Enzyme/Protease
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  3. LEI-401

LEI-401 

Cat. No.: HY-131181
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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.

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LEI-401 Chemical Structure

LEI-401 Chemical Structure

CAS No. : 2393840-15-6

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Description

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].

In Vitro

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: Male 7–12-week-old C57BL/6J mice[1]
Dosage: 30 mg/kg
Administration: I.p.
Result: Produced a significant increase in freezing as compared to vehicle.
Animal Model: C57BL/6J mice[1]
Dosage: 10 mg/kg
Administration: P.o. (Pharmacokinetic Analysis)
Result: The t1/2, Cmax, tmax, AUClast, and F values were 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively.
Molecular Weight

421.54

Formula

C₂₄H₃₁N₅O₂

CAS No.

2393840-15-6

SMILES

O=C(C1=NC(N2C[[email protected]](C3=CC=CC=C3)CCC2)=NC(N4C[[email protected]@H](O)CC4)=C1)NCC5CC5

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

LEI-401LEI401LEI 401PhospholipaseemotionalbehaviorCNSneuronalcellsHEK293Tbrain-penetrantHPAaxissignalingInhibitorinhibitorinhibit

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