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Monoacylglycerol Lipase Inhibitor 21
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Monoacylglycerol Lipase Inhibitor 21图片
CAS NO:1643657-35-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Cas No.1643657-35-5
别名MAGL Inhibitor 21,MGL Inhibitor 21
化学名1,3-benzodioxol-5-ylmethyl ester [1,1'-biphenyl]-4-hexanoic acid
Canonical SMILESO=C(OCC1=CC(OCO2)=C2C=C1)CCCCCC(C=C3)=CC=C3C4=CC=CC=C4
分子式C26H26O4
分子量402.5
溶解度≤21mg/ml in ethanol;0.5mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki: 0.4 μM for MAGL

Monoacylglycerol Lipase Inhibitor 21 is an inhibitor of monoacylglycerol lipase (MAGL) and FAAH.

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA) are biologically active lipids involved in various synaptic processes including activation of cannabinoid receptors. Fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) mediate the hydrolysis of AEA and 2-AG, respectively.

In vitro: A previous study confirmed that Monoacylglycerol Lipase Inhibitor 21 could inhibit MAGL in a reversible manner. Moreover, the kinetic studies indicated that Monoacylglycerol Lipase Inhibitor 21 acted as a noncompetitive inhibitor. In addition, Monoacylglycerol Lipase Inhibitor 21 did not bind CB1 or CB2 receptors. Furthermore, the selectivity of Monoacylglycerol Lipase Inhibitor 21 was studied in a broad panel that includes a variety of receptors and enzymes, and the results showed that Monoacylglycerol Lipase Inhibitor 21 did not inhibit significantly any of the analyzed targets [1].

In vivo: Multiple sclerosis (MS) mouse model was used to evaluated the in-vivo efficacy of Monoacylglycerol Lipase Inhibitor 21. Treatment started at day 6 post-immunization and consisted of daily injections of Monoacylglycerol Lipase Inhibitor 21 (5 mg/kg, i.p.) for the following 21 days. Results showed that the administration of Monoacylglycerol Lipase Inhibitor 21 could clearly ameliorate the progression of the disease, as assessed by the significantly lower clinical score in the MS model. This improvement correlated with an increase of the 2-AG levels in the spinal cord of treated animalsand with evident changes at the histological level, as Monoacylglycerol Lipase Inhibitor 21 was able to significantly decrease leukocyte infiltration and microglial response, prevent axonal damage, as well as partially restore myelin morphology in EAE mice [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Hernández-Torres, G. ,Cipriano, M.,Hedén, E., et al. A reversible and selective inhibitor of monoacylglycerol lipase ameliorates multiple sclerosis. Angewandte Chemistry International Edition English 53(50), 13765-13770 (2014).