Selectively and reversibly blocks MAGL activity (IC50s = 0.18 and 59 µM for MAGL and FAAH in mouse brain

Monoacylglycerol Lipase Inhibitor 21 – 50 mg

Brand:
Cayman
CAS:
1643657-35-5
Storage:
-20
UN-No:
Non-Hazardous - /

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG; Item No. 62160) and arachidonoyl ethanolamide (AEA; Item No. 90050) are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid (CB) receptors. Fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) mediate the hydrolysis of AEA and 2-AG, respectively. MAGL inhibitor 21 selectively binds to MAGL (Ki = 0.4 µM) and reversibly blocks the enzyme’s activity in mouse brain with an IC50 value of 0.18 µM.{27369} Comparatively, MAGL inhibitor 21 is reported to inhibit FAAH activity in mouse brain with an IC50 value of 59 µM.{37369} This compound does not bind CB1 or CB2 receptors and does not inhibit the related serine hydrolases ABHD6 and ABHD12 (Kis > 10 µM).{27369} In a mouse model of multiple sclerosis, 5 mg/kg of MAGL inhibitor 21 has been used to ameliorate progression of the disease without producing detrimental CB1-mediated effects.{27369}  

 

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Description

Selectively and reversibly blocks MAGL activity (IC50s = 0.18 and 59 µM for MAGL and FAAH in mouse brain, respectively); does not inhibit ABHD6, ABHD12, CB1, or CB2 receptors (Kis > 10 µM); used to ameliorate disease progression in a mouse model of multiple sclerosis

Formal name: [1,1’-biphenyl]-4-hexanoic acid, 1,3-benzodioxol-5-ylmethyl ester

Synonyms:  MAGL Inhibitor 21|MGL Inhibitor 21

Molecular weight: 402.5

CAS: 1643657-35-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids

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