1402612-55-8

生物活性：KT109 是一种有效的，选择性二酰甘油脂肪酶-β (DAGLβ) 抑制剂，IC₅₀ 为 42 nM。KT109 对 DAGLβ 的选择性比 DAGLα 高约 60 倍。KT109 对 PLA2G7 有抑制活性 (IC₅₀=1 µM)。KT109 不影响 FAAH、MGLL、ABHD11 和胞质磷脂酶 A2 (cPLA2 或 PLA2G4A) 的活性。KT109 可以扰乱参与巨噬细胞炎症反应的脂质网络，并降低小鼠腹腔巨噬细胞中 2-花生四烯酸甘油 (2-AG)、花生四烯酸和类花生酸。

KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC₅₀ of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC₅₀=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-arachidonoylglycerol (2-AG), arachidonic acid and eicosanoids in mouse peritoneal macrophages^[1].