KT109 是一种有效的异构体选择性二酰基甘油脂肪酶-β (DAGLβ) 抑制剂，IC50 为 42 nM。
| Cas No. | 1402612-55-8 |
| Canonical SMILES | O=C(N1N=NC(C2=CC=C(C3=CC=CC=C3)C=C2)=C1)N4C(CC5=CC=CC=C5)CCCC4 |
| 分子式 | C27H26N4O |
| 分子量 | 422.5 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. KT109 is a selective inhibitor of DAGLβ with an IC50 value of 42 nM. It demonstrates ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11. KT109 has been shown to disrupt the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages. |
