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KT109
产品别名
1402612-55-8
KT109
(4-([1,1′-Biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)(2-benzylpiperidin-1-yl)methanone
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C27H26N4O |
| Molecular weight | 422.52 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | KT109 is a potent and selective inhibitor of Diacylglycerol lipase DAGLβ. Diacylglycerol lipases DAGLα and DAGLβ are serine hydrolases that biosynthesize the endocannabinoid 2-arachidonoylglycerol (2-AG). A lack of selective inhibitors has hampered study of these lipases. KT109 is a potent and selective DAGLβ inhibitor with an IC50 of 42 nM, ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling. KT109 shows some inhibitory activity against PLA2G7 (IC50 = 1 μM) but no inhibitory activity against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC50 = 16 nM) can be controlled for by use of the related compound, KT195, a potent (IC50 = 10 nM) and selective ABHD6 inhibitor with negligible activity against DAGLβ. KT109 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages. |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 10 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | O=C(N1CCCCC1Cc2ccccc2)n3cc(nn3)-c4ccc(cc4)-c5ccccc5 |
| packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
| Pictograms【象形图】 | GHS07 |
| Signal word【警示用语：】 | Warning |
| Hazard Statements | H302 - H413 |
| Precautionary Statements | P273 - P301 + P312 + P330 |
| Hazard Classifications【危险分类】 | Acute Tox. 4 Oral - Aquatic Chronic 4 |
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
