1. Metabolic Enzyme/Protease
  2. MAGL

MAGL

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.

MAGL 相关产品 (8):

Cat. No. Product Name Effect Purity
  • HY-15249
    JZL 184 Inhibitor
    JZL 184是MAGL的有效选择性抑制剂,IC50值为8nM,对FAAH的IC50值为4uM。
  • HY-15250
    JZL195 Inhibitor 99.75%
    JZL195是一高效、选择性FAAH/MAGL双重抑制剂,对小鼠脑FAAH和MAGL的IC50值分别为13nM和19nM。
  • HY-100337
    WWL70 Inhibitor 99.98%
    WWL70 是一个选择性的 α/β 水解酶结构域 6 (ABHD6) 抑制剂,其 IC50 值为 70 nM。
  • HY-18977
    KML29 Inhibitor 99.21%
    KML29是一种有效的选择性MAGL抑制剂, 抑制人, 小鼠, 和大鼠脑蛋白酶时, IC50 分别为5.9, 15, 和 43 nM。
  • HY-12332
    JW 642 Inhibitor
    JW 642是一高效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。
  • HY-114157
    DO-264 Inhibitor
    DO-264 是一个具有体内活性的、自水解酶结构域 12 (ABHD12) 的抑制剂,其 IC50 值为 11 nM。
  • HY-117632
    ABX-1431 Inhibitor
    ABX-1431是一种高效,选择性和口服可用的CNS-渗透性单酰基甘油脂肪酶 (MAGL)抑制剂,IC50 为14 nM。
  • HY-108613
    JJKK 048 Inhibitor
    JJKK 048 是一种超高效且有高选择性的单酰甘油脂肪酶 (MAGL) 抑制剂。
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