Home>>Lipids>> Endocannabinoid/Endocannabinoid-like>>LEI-106

LEI-106 Sale

目录号 : GC44049

A potent inhibitor of sn-1 DAGLα

LEI-106 Chemical Structure

Cas No.:1620582-23-1

规格 价格 库存 购买数量
1mg
¥616.00
现货
5mg
¥1,850.00
现货
10mg
¥3,289.00
现货
25mg
¥7,195.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. LEI-106 is a potent in vitro inhibitor of sn-1 DAGLα (IC50 = 18 nM). It blocks the hydrolysis of sn-1-oleoyl-2-AG, the natural substrate of DAGLα, with a Ki 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 (Ki = 0.8 µM).

Chemical Properties

Cas No. 1620582-23-1 SDF
Canonical SMILES OC(CN(S(C1=CC=C(OC(C)(C)CC2)C2=C1)(=O)=O)CC(C=C3)=CC=C3OC4=CC=CC=C4)=O
分子式 C26H27NO6S 分子量 481.6
溶解度 DMF: 50 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 30 mg/ml,Ethanol: 0.1 mg/ml 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.0764 mL 10.3821 mL 20.7641 mL
5 mM 0.4153 mL 2.0764 mL 4.1528 mL
10 mM 0.2076 mL 1.0382 mL 2.0764 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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 g 每只动物给药体积 ul 动物数量
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GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

Research Update

Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6

J Med Chem 2014 Aug 14;57(15):6610-22.PMID:24988361DOI:10.1021/jm500681z

sn-1-Diacylglycerol lipase α (DAGL-α) is the main enzyme responsible for the production of the endocannabinoid 2-arachidonoylglycerol in the central nervous system. Glycine sulfonamides have recently been identified by a high throughput screening campaign as a novel class of inhibitors for this enzyme. Here, we report on the first structure-activity relationship study of glycine sulfonamide inhibitors and their brain membrane proteome-wide selectivity on serine hydrolases with activity-based protein profiling (ABPP). We found that (i) DAGL-α tolerates a variety of biaryl substituents, (ii) the sulfonamide is required for inducing a specific orientation of the 2,2-dimethylchroman substituent, and (iii) a carboxylic acid is essential for its activity. ABPP revealed that the sulfonamide glycine inhibitors have at least three off-targets, including α/β-hydrolase domain 6 (ABHD6). Finally, we identified LEI-106 as a potent, dual DAGL-α/ABHD6 inhibitor, which makes this compound a potential lead for the discovery of new molecular therapies for diet-induced obesity and metabolic syndrome.