| CAS NO: | 915191-42-3 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 1mg | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| Cas No. | 915191-42-3 |
| 化学名 | N-[[[4-(5,9-diethoxy-6,8-dihydro-6-oxo-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methyl]sulfonyl]-2-methoxy-benzeneacetamide |
| Canonical SMILES | O=C1N(C2=C(C)C=C(CS(NC(CC3=CC=CC=C3OC)=O)(=O)=O)C=C2)CC4=C(OCC)C5=C(C=CC=N5)C(OCC)=C41 |
| 分子式 | C32H33N3O7S |
| 分子量 | 603.7 |
| 溶解度 | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| 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 | MF498 is a novel and selective EP4 antagonist [1]. Prostaglandin E2 receptors (EP) are G-protein coupled receptors (GPCRs) and functions with the binding of Prostaglandin (PG) E2. The EPs exhibit differences in signal transduction, tissue localization, and regulation of expression. The EP4 receptor is over-expressed in human prostate cancer tissue [2]. In vitro: MF498 was a selective EP4 receptor antagonist with the Ki of 0.7 nM while the Ki >1 μM for other EP receptors. In HEK293 cells expressing human EP4 receptor, MF498 inhibited EP ligand-induced activity with an IC50 value of 1.7 nM [1]. In vivo: In rodent models of rheumatoid and osteoarthritis, MF498 inhibited inflammation without gastrointestinal toxicity, the ED50 values was as low as 0.02 mg/kg/day[1].In adjuvant-induced arthritis (AIA) rat model for rheumatoid arthritis (RA), MF498 inhibited inflammation. In addition, MF498 was effective in relieving OA-like pain in guinea pigs. In rat models of gastrointestinal toxicity, MF498 was well tolerated, causing no mucosal leakage or erosions. In a furosemide-induced diuresis model, MF498 reduced furosemide-induced natriuresis by 50% [3]. References: |
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