1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. MAGL

MAGL (单酰甘油酯酶)

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 (10):

Cat. No. Product Name Effect Purity
  • HY-15249
    JZL 184 Inhibitor 98.20%
    JZL 184 是一种有效的,选择性的且不可逆的 MAGL 抑制剂,可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC50 为 8 nM)。JZL 184 对 MAGL 的选择性比 FAAH 高 300 倍以上。
  • 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-108613
    JJKK 048 Inhibitor >98.0%
    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。
  • HY-120177
    KT182 Inhibitor >99.0%
    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-114926
    KT185 Inhibitor >99.0%
    KT185 是口服有效的、能透过血脑屏障的ABHD6 的选择性抑制剂,其在 Neuro2A 细胞中测得的 IC50 值为0.21 nM。
  • HY-120215
    KT203 Inhibitor >98.0%
    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-N0313
    Euphol Inhibitor 98.82%
    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。
  • HY-103463
    SA57 Inhibitor >99.0%
    SA57 是一种有效的选择性 FAAH 抑制剂,对小鼠和人类 FAAHIC50 分别为 3.2 nM 和 1.9 nM。SA57 还抑制 2-花生四烯酸甘油水解酶 MAGL (对小鼠和人类 MAGLIC50 分别为 410 nM 和 1.4 μM)和小鼠 α/β-水解酶结构域蛋白 6 (mABHD6; IC50 为 850 nM),但不抑制其他脑丝氨酸水解酶。
  • 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。
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