human magl

SA57 is a potent, selective inhibitor of FAAH(IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH).

JZP-430 是不可逆的、高度选择性的 α β 水解酶结构域 6 抑制剂，能够靶向抑制人类 ABHD6 ，其 IC50=44 nM。

JW 642 是一种高效的MAGL 抑制剂，对小鼠、大鼠和人源脑细胞膜上MAGL 的IC50值分别为7.6nM、14nM 和3.7nM。

SAR127303 is an effective covalent inhibitor of MAGL. SAR127303 behaves as a selective and competitive inhibitor of mouse and human MAGL.

JZP-361 是一种特异性 MAGL 抑制剂，对人重组 MAGL、人重组 FAAH 和人 hABHD6 的 IC50 分别为 46 nM、7.24 μM 和 1.79 μM。 JZP-361 具有抗组胺活性。 JZP-361可用于哮喘研究。

OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microM

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URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 value of 32 μM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 value of 3.8 μM. It does not inhibit COX-1 or COX-2 at concentrations up to 100 μM. Inhibition of MAGL hydrolysis of 2-arachidonoyl glycerol (2-AG) is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.

KML29 是一种口服具有活性的、高度选择性的不可逆 MAGL 抑制剂，其对小鼠、大鼠和人的 IC50值分别为15 nM、43 nM 和 5.9 nM。它对 FAAH 在内的其他中心和外周丝氨酸水解酶的交叉反应极小。

MAGLi 432 是一种有效的、高度选择性的、非共价的、可逆的 (MAGL) 抑制剂。MAGLi 432 能够高亲和力的结合 MAGL 活性位点，其 IC50 值为 4.2 nM (human enzyme) 和 3.1 nM (mouse enzyme)。MAGLi 432 能够用于研究慢性炎症、多发性硬化症、血脑屏障功能障碍、阿尔茨海默病和帕金森病等神经系统疾病。

MAGL-IN-8 (compound 13) 是一种针对 hMAGL 的高选择性可逆抑制剂，其IC50值为2.5 ± 0.4 nM。

AKU-005 是一种针对FAAH和MAGL的双重抑制剂，其对大鼠FAAH和人类FAAH的抑制常数(IC50)分别为63 nM和389 nM。该化合物在探索三叉神经痛觉过敏方面显示出研究潜力。