2393840-15-6

2393840-15-6 structure
2393840-15-6 structure
  • Name: LEI-401
  • Chemical Name: LEI-401
  • CAS Number: 2393840-15-6
  • Molecular Formula: C24H31N5O2
  • Molecular Weight: 421.54
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
  • Create Date: 2020-08-07 11:18:38
  • Modify Date: 2024-01-16 19:04:59
  • 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].

Name LEI-401
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].
Related Catalog
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.
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.

Molecular Formula C24H31N5O2
Molecular Weight 421.54