1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. 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 (14):

Cat. No. Product Name Effect Purity
  • HY-15249
    JZL 184 Inhibitor 98.20%
    JZL 184是有效,选择性和不可逆的单酰基甘油脂肪酶 (MAGL) 抑制剂,抑制MAGL 和小鼠脑膜中的脂肪酸酰胺水解酶的 IC50 值分别为8 nM 和 4 μM。
  • 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-15250
    JZL195 Inhibitor 99.75%
    JZL195 是一种有效选择的脂肪酸酰胺水解酶 (FAAH) 和单酰甘油脂肪酶 (MAGL) 双重抑制剂,IC50s 分别为 2 和 4 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-117632
    ABX-1431 Inhibitor 99.96%
    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-114926
    KT185 Inhibitor
    KT185 是口服有效的、能渗透大脑的ABHD6 的选择性抑制剂,其在 Neuro2A 细胞中测得的 IC50 值为0.21 nM。
  • HY-111538
    MAGL-IN-1 Inhibitor
    MAGL-IN-1是有效,选择性,可逆的单酰甘油脂肪酶 (MAGL)抑制剂,IC50为80 nM。
  • HY-111512
    PF-06795071 Inhibitor
    PF-06795071 是一种有效的选择性共价 MAGL 抑制剂,IC50 为 3 nM。
  • HY-12332
    JW 642 Inhibitor 99.70%
    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-120177
    KT182 Inhibitor
    KT182 是一个有效的、α/β 水解酶结构域 6 (ABHD6) 的选择性抑制剂,其在 Neuro2A 细胞中测得的 IC50 值为0.24 nM。
  • HY-120215
    KT203 Inhibitor
    KT203 是一个有效的、α/β 水解酶结构域 6 (ABHD6) 的选择性抑制剂,其在 Neuro2A 细胞中测得的 IC50 值为0.31 nM。
  • HY-101457
    JZP-430 Inhibitor >99.0%
    JZP-430 是一种有效的、高度选择性的、不可逆的 α/β 水解酶结构域 6 (ABHD6) 抑制剂,靶向抑制人类 ABHD6 的 IC50 值为 44 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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