R-59-949 是泛二酰基甘油激酶 (DGK) 抑制剂，IC50 为 300 nM。 R-59-949 强烈抑制 I 型 DGK α 和 γ 的活性并适度减弱 II 型 DGK θ 和 κ 的活性。 R-59-949 通过提高内源性配体二酰基甘油的水平来激活蛋白激酶 C (PKC)。
| Cas No. | 120166-69-0 |
| 化学名 | 3-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone |
| Canonical SMILES | S=C1N(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)/C4=CC=C(F)C=C4)C(C5=CC=CC=C5N1)=O |
| 分子式 | C28H25F2N3OS |
| 分子量 | 489.6 |
| 溶解度 | DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 1 mg/ml |
| 储存条件 | Store at -20°C, stored under nitrogen |
| 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 | R-59-949 is an inhibitor of diacylglycerol kinase α (DGK-α) with an IC50 value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate. DGK-α inhibition with R-59-949 increases diacylglycerol-dependent PKC activity, serotonin secretion, and aggregation of thrombin-stimulated platelets. R-59-949 inhibits DGK-α activity induced by platelet-derived growth factor (PDGF) in intact vascular smooth muscle cells (VSMCs). It inhibits high K+- and glucose-induced insulin secretion in MIN6 pancreatic β-cells in a dose-dependent manner. In vivo, administration of R-59-949 prevents retinal neovascularization in a mouse model of oxygen-induced retinopathy. |
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