计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC 50 of 27 nM. LEI-401 modulates emotional behavior in mice.
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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LEI-401 (30 mg/kg; i.p.) diminishes fear extinction in mice . LEI-401 also activates HPA axis signaling . LEI-401 (10 mg/kg; p.o.) treatment shows the t 1/2 , C max , t max , AUC last , and F values of 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively . LEI-401 (30 mg/kg; i.p.) treatment show the C max , t max , AUC last , and F values of 10300 ng/mL, 1 hour, 38600 h*ng/mL, and 48%, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male 7–12-week-old C57BL/6J mice Dosage: 30 mg/kg Administration: I.p. Result: Produced a significant increase in freezing as compared to vehicle. Animal Model: C57BL/6J mice Dosage: 10 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The t 1/2 , C max , t max , AUC last , and F values were 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively.
规格
规格或纯度
10mM in DMSO
英文名称
LEI-401
生化机理
LEI-401 是一种具有选择性和中枢神经系统活性的 NAPE-PLD（N-acylphosphatidylethanolamine phospholipase D）抑制剂，其 IC 50 为 27 nM。LEI-401 可调节小鼠的情绪行为。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1C[C@H](CN(C1)C2=NC(=CC(=N2)N3CC[C@@H](C3)O)C(=O)NCC4CC4)C5=CC=CC=C5
PubChem CID
分子量
421.54
技术文档
高级数据
关联靶点（人）
NAPEPLD
Tchem
N-酰基磷脂酰乙醇胺水解磷脂酶D(N-acyl-phosphatidylethanolamine-hydrolyzing phospholipase D)
(0 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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