Mono<wbr/>acylglycerol Lipase Inhibitor 21

Monoacylglycerol Lipase Inhibitor 21

CAT N°: 16964
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From 91.00 77.35

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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