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Monoacylglycerol Lipase Inhibitor 21 Sale

(Synonyms: MAGL Inhibitor 21,MGL Inhibitor 21) 目录号 : GC12031

A reversible blocker of 2-AG hydrolysis

Monoacylglycerol Lipase Inhibitor 21 Chemical Structure

Cas No.:1643657-35-5

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Sample solution is provided at 25 µL, 10mM.

Description

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).

化学性质

Cas No. 1643657-35-5 SDF
别名 MAGL Inhibitor 21,MGL Inhibitor 21
化学名 1,3-benzodioxol-5-ylmethyl ester [1,1'-biphenyl]-4-hexanoic acid
Canonical SMILES O=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°C
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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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4845 mL 12.4224 mL 24.8447 mL
5 mM 0.4969 mL 2.4845 mL 4.9689 mL
10 mM 0.2484 mL 1.2422 mL 2.4845 mL
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