Monoacylglycerol Lipase Inhibitor 21
货号：
16964-100mg 基本售价：
9408.0 元 规格：
100 mg
产品信息
概述| 货号 | 16964-100mg |
| 描述 | 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.1 Comparatively, MAGL inhibitor 21 is reported to inhibit FAAH activity in mouse brain with an IC50 value of 59 µM.2 This compound does not bind CB1 or CB2 receptors and does not inhibit the related serine hydrolases ABHD6 and ABHD12 (Kis > 10 µM).1 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.1 |
| 别名 | MAGL Inhibitor 21;MGL Inhibitor 21; |
性能| 供应商 | Cayman |
| 应用文献 |
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).
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| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 402.5 |
| 分子式 | C26H26O4 |
| CAS号 | 1643657-35-5 |
| 稳定性 | ≥ 2 years |
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