LEI-106 - CAS:1620582-23-1

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LEI-106

目录号 : KCM11803 CAS No. : 1620582-23-1 纯度 : ≥98%

Data Sheet 产品使用指南

In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; ) by attacking DAG at the sn-1 position. LEI-106 is a potent in vitro inhibitor of sn-1 DAGLα (IC = 18 nM). It blocks the hydrolysis of sn-1-oleoyl-2-AG, the natural substrate of DAGLα, with a K value of 0.7 µM. LEI-106 inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6 in mouse brain membrane homogenates and in HEK293T cell membrane preparations (K = 0.8 µM).

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

LEI-106 is a dual ABHD6 and DAGL-α inhibitor, with a Ki of 0.8 μM for ABHD6, and an IC50 of 18 nM and a Ki of 0.7 μM for DAGL-α. LEI-106 blocks the synthesis of 2-arachidonoylglycerol, reduces the level of endothelial cell-derived 2-arachidonoylglycerol, without altering the levels of cannabinoids and diacylglycerol. LEI-106 is applicable to research related to diet-induced obesity and metabolic syndrome[1].

IC₅₀&Target

DAGLα DAGLα ABHD6

18 nM (IC50) 0.7 μM (Ki) 0.8 μM (Ki)

体外研究

LEI-106 (compound 15) potently inhibits human DAGL-α activity in a cell-free HEK293 membrane system, with an IC50 of 18 nM in colorimetric assays and a Ki of 0.7 μM against the natural substrate [1].
LEI-106 (20 μM; 20 min) potently inhibits the endogenous DAGL-α activity in mouse meningeal homogenate, with an IC50 of 124 nM, and also acts as an inhibitor of ABHD6 in this system [1].
LEI-106 (processed for 30 minutes) potently inhibits human ABHD6 activity in cell-free HEK293T membranes, with a Ki value of 0.8 μM for the natural substrate 2-AG [1].
LEI-106 (1.3 mM; 15 min) significantly reduced 2-AG levels in bEnd.3 mouse brain endothelial cells without altering AEA levels [2].
LEI-106 (650 μM-1.3 mM; 15 min) significantly enhances PKC activity in bEnd.3 mouse brain endothelial cells [2].
LEI-106 (650 μM-1.3 mM; 15 min) induces VE-cadherin fragmentation in mouse brain endothelial cells bEnd.3, and a concentration of 1.3 mM further reduces the levels of full-length VE-cadherin, claudin-5, and ZO-1; Rho kinase inhibition alleviates VE-cadherin fragmentation, whereas calpain or PKC inhibition has no such effect [2].
LEI-106 (650-1.3 mM; 2 min) significantly increased intracellular calcium levels in bEnd.3 mouse brain endothelial cells [2].
LEI-106 (650 μM; 15 min) significantly alters the phosphorylated proteome of bEnd.3 murine brain endothelial cells, involving changes in mRNA processing, cytoskeleton assembly, and Rho GTPase signaling pathways [2].

ELISA Assay

Cell Line:	bEnd.3 mouse brain endothelial cells
Concentration:	650 μM; 1.3 mM
Incubation Time:	15 min
Result:	Caused no significant change in DAG levels compared to vehicle control at either concentration. Significantly increased PKC activity at both concentrations compared to vehicle.

分子式

C₂₆H₂₇NO₆S

分子量

481.6

CAS号

1620582-23-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO: 50 mg/mL (103.83 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0766 mL	10.3829 mL	20.7658 mL
5 mM	0.4153 mL	2.0766 mL	4.1532 mL
10 mM	0.2077 mL	1.0383 mL	2.0766 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。

纯度： ≥98%

Data Sheet

产品使用指南

[1]. Janssen FJ, et al. Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6. J Med Chem. 2014;57(15):6610-6622.

[2]. Levine AA, et al. Depletion of Endothelial-Derived 2-AG Reduces Blood-Endothelial Barrier Integrity via Alteration of VE-Cadherin and the Phospho-Proteome. Int J Mol Sci. 2023;25(1):531. Published 2023 Dec 30.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器