Diflapolin 是一种高活性的双重 5-脂氧合酶激活蛋白 (FLAP)/可溶性环氧化物水解酶 (sEH) 抑制剂，具有显着的抗炎功效和高靶向选择性。
| Cas No. | 724453-98-9 |
| 别名 | 双黄素 |
| Canonical SMILES | CC1=C(NC(NC2=CC(Cl)=C(Cl)C=C2)=O)C=CC(OCC3=NC4=C(C=CC=C4)S3)=C1 |
| 分子式 | C22H17Cl2N3O2S |
| 分子量 | 458.4 |
| 溶解度 | DMF: 2.5mg/mL,DMSO: 1.6mg/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 | Diflapolin is a dual inhibitor of 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH). It inhibits formation of the 5-lipoxygenase (5-LO) products leukotriene B4 and 5-HpETE in isolated human monocytes and neutrophils (IC50s = 30 and 170 nM, respectively) and inhibits the epoxide hydrolase activity of sEH with an IC50 value of 20 nM in a cell-free assay. It is selective for FLAP and sEH over other arachidonic acid metabolism enzymes, including 5-LO, LTC4 synthase, mPGES-1, COX-1, or COX-2 in cell-free assays, as well as 12- and 15-LO in neutrophils. Diflapolin (1, 3, and 10 mg/kg) decreases inflammation in a mouse model of peritonitis induced by zymosan, reducing the production of LTB4 and LTC4 and inhibiting leukocyte recruitment. |
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