产品说明
包装
5, 25 mg in glass bottle
生化/生理作用
KT172 is a Diacylglycerol lipase (DAGL) inhibitor selective for 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. KT172 is a new potent and selective DAGLβ inhibitor with an IC50 of 60 nM for recombinant DAGLβ vs 140 nM for DAGLα, although it is not active against DAGLα in vivo, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling or against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC50 values of 5 nM) can be controlled for by use of the related compounds, KT195 SML1308 or KT185 SML1249, potent and selective ABDH6 inhibitors with negligible activity against DAGLβ. KT172 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.
基本信息
| 经验(实验)分子式 | C28H28N4O2 |
| 分子量 | 452.55 |
| MDL编号 | MFCD26960820 |
| PubChem化学物质编号 | 329826017 |
| NACRES | NA.77 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 20 mg/mL, clear |
| 储存温度 | 2-8℃ |
| SMILES string | O=C(N1N=NC(C2=CC=C(C3=C(OC)C=CC=C3)C=C2)=C1)N4CCCCC4CC5=CC=CC=C5 |
| InChI | 1S/C28H28N4O2/c1-34-27-13-6-5-12-25(27)22-14-16-23(17-15-22)26-20-32(30-29-26)28(33)31-18-8-7-11-24(31)19-21-9-3-2-4-10-21/h2-6,9-10,12-17,20,24H,7-8,11,18-19H2,1H3 |
| InChI key | MXVVJNJNDCJCFS-UHFFFAOYSA-N |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
