Monoacylglycerol lipase (MGL) is a 33 kDa serine hydrolase that catalyses the hydrolysis of monoacylglycerols to their corresponding fatty acids. The enzyme is found both in the brain and in peripheral tissues such as the kidney, ovary, testis, adrenal gland, adipose tissue and heart. The three-dimensional structure of MGL has been elucidated by X-ray crystallography, and the enzyme has been shown to be a dimeric molecule with amphitropic properties, that is, it can exist both in a soluble form and associated with the membrane lipid bilayers. Mutagenesis studies have demonstrated the importance of the catalytic triad of ser122, asp239 and his269 that the enzyme shares with other enzymes in the α/β hydrolase superfamily. The substrate is recruited via a wide hydrophobic tunnel, where it can then interact with the catalytic triad at the end of the tunnel.
MGL inhibitors have lagged behind, but have a potential advantage over FAAH inhibitors in terms of eCB specificity of action given that the N-acylethanolamines are a class of compounds with multiple biological actions.
- Cat.No. 产品名称 Information
- GC62821 AA38-3 AA38-3, a serine hydrolase (SH) inhibitor, can inhibit three SHs, ABHD6, ABHD11, and FAAH.
- GC19412 ABX-1431 An inhibitor of MAGL
- GC34327 DO-264 An ABHD12 inhibitor
- GC38638 Euphol Euphol 是一种四环三萜醇，是从 Euphorbia tirucalli 的汁液中分离出来的，具有抗炎和免疫调节作用，具有口服活性。 Euphol 通过一种可逆机制抑制单酰基甘油脂肪酶 (MGL) 的活性，IC50=315 nM。 外周 MGL 抑制可调节内源性大麻素系统从而阻止炎症性疼痛的发展。
- GC10162 JJKK 048 JJKK 048 是一种超强效和高选择性的单酰基甘油脂肪酶 (MAGL) 抑制剂。
- GC12693 JZL 195 A potent inhibitor of both FAAH and MAGL
- GC14390 JZL184 A potent and selective inhibitor of MAGL
- GC34640 JZP-430 An ABHD6 inhibitor
An inhibitor of MAGL
- GC16756 KT182 A potent inhibitor of ABHD6
- GC36401 KT185 An inhibitor of ABHD6
- GC13763 KT203 A potent inhibitor of ABHD6
- GC63055 MAGL-IN-4 MAGL-IN-4 是一种口服有效，选择性和可逆的单酰基甘油脂肪酶 (MAGL) 抑制剂，IC50 为 6.2 nM。MAGL-IN-4 可以穿透血脑屏障 (BBB)。MAGL-IN-4 主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油 (2-AG) 水平来增强内源性大麻素信号。
- GC14079 MJN110 A selective MAGL inhibitor
- GC17855 SA 57 An inhibitor of FAAH, MAGL, and ABHD6
- GC15074 WWL 70 A selective inhibitor of ABHD6