Monoacylglycerol Lipase Inhibitor 21

- Overview
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    Background
    
    Ki: 0.4 μM for MAGLMonoacylglycerol 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.
- Properties
  - Alternative Name
    
    MAGL Inhibitor 21,MGL Inhibitor 21; 1,3-benzodioxol-5-ylmethyl ester [1,1'-biphenyl]-4-hexanoic acid
    
    CAS Number
    
    1643657-35-5
    
    Molecular Formula
    
    C26H26O4
    
    Molecular Weight
    
    402.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤21mg/ml in ethanol;0.5mg/ml in DMSO;30mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Monoacylglycerol Lipase Inhibitor 21

Monoacylglycerol Lipase Inhibitor 21

Background

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