| Description | LEI-401 is a selective and potent NAPE-PLD inhibitor that crosses the blood-brain barrier (IC50: 27 nM).LEI-401 reduces the level of n-acylethanolamines (NAEs) in the brain of free-ranging mice and modulates their emotional behaviour. |
| In vitro | 在转染了hNAPE-PLD的HEK293T细胞中，LEI-401(0.04-20 μM；30分钟)剂量依赖性地减少NAPE-PLD标记，IC50为0.86 μM。LEI-401降低了Neuro-2a细胞中的NAE水平，但在NAPE-PLD KO细胞中没有降低[1]。 |
| In vivo | LEI-401在C57BL/6J小鼠血浆中的体内药代动力学剖析，通过腹腔注射(i.p., 30 mg/kg)、口服(p.o., 10 mg/kg)或静脉注射(i.v., 1 mg/kg)给药。结果显示LEI-401是一种体内有效的NAPE-PLD抑制剂，可用于研究其生理作用。[1]。 |
| Target activity | NAPE-PLD:0.86 μM |
| Synonyms | LEI 401 |
| molecular weight | 421.54 |
| Molecular formula | C24H31N5O2 |
| CAS | 2393840-15-6 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (189.78 mM), Sonication is recommended. |
| 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. |