LEI-401,99.79%

产品编号:Bellancom-131181| CAS NO:2393840-15-6| 分子式:C24H31N5O2| 分子量:421.54

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-131181
1500.00 杭州 北京(现货)
Bellancom-131181
2200.00 杭州 北京(现货)
Bellancom-131181
4500.00 杭州 北京(现货)
Bellancom-131181
7700.00 杭州 北京(现货)
Bellancom-131181
13500.00 杭州 北京(现货)

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LEI-401

产品介绍 LEI-401 是一种首创的、选择性的、通过血脑屏障的 NAPE-PLD (N-酰基磷酰乙醇胺磷脂酶 D) 抑制剂,IC50 为 27 nM。LEI-401 对小鼠情绪行为的调节。
生物活性

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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 t1/2, Cmax, tmax, AUClast, 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 Cmax, tmax, AUClast, and F values of 10300 ng/mL, 1 hour, 38600 h*ng/mL, and 48%, respectively.

西域 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 t1/2, Cmax, tmax, AUClast, and F values were 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively.
体内研究

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 t1/2, Cmax, tmax, AUClast, 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 Cmax, tmax, AUClast, and F values of 10300 ng/mL, 1 hour, 38600 h*ng/mL, and 48%, respectively.

西域 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 t1/2, Cmax, tmax, AUClast, and F values were 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively.
性状Solid
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (237.23 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3723 mL 11.8613 mL 23.7225 mL
5 mM 0.4745 mL 2.3723 mL 4.7445 mL
10 mM 0.2372 mL 1.1861 mL 2.3723 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.93 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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