| 货号 | 15973-25mg |
| 描述 | Prostaglandin E2(PGE2; Item No. 14010) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis.1,2,3 MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).4 In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.4 In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Li, M.,Thompson, D.D. and Paralkar, V.M. Prostaglandin E2 receptors in bone formation. International Orthopaedics 31, 767-772 (2007). 2.Hawcroft, G.,Ko, C.W.S. and Hull, M.A. Prostaglandin E2-EP4 receptor signalling promotes tumorigenic behaviour of HT-29 human colorectal cancer cells. Oncogene 26, 3006-3019 (2007). 3.Babaev, V.R.,Chew, J.D.,Ding, L., et al. Macrophage EP4 deficiency increases apoptosis and suppresses early atherosclerosis. Cell Metabolism 8, 492-501 (2008). 4.Clark, P.,Rowland, S.E.,Denis, D., et al. MF498 [N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis. Journal of Pharmacology and Experimental Therapeutics 325(2), 425-434 (2008). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 603.7 |
| 分子式 | C32H33N3O7S |
| CAS号 | 915191-42-3 |
| 稳定性 | ≥ 2 years |
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