| 货号 | 10010428-250mg |
| 描述 | Prostaglandin E2(PGE2) 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, cancer, and atherosclerosis.1,2,3 CJ-42794 is a selective antagonist of EP4(Ki = 3.16 nM) that less potently binds EP2(Ki = 631 nM) and has no affinity for EP1 or EP3.4,5 It has minimal effect on numerous other receptors, enzymes, or channels.5 Unlike general inhibitors of PGE2 synthesis, CJ-42794 does not cause damage to rat gastrointestinal mucosa.4 Instead, it delays the healing of gastric ulcers in mice and rats, suppressing the upregulation of VEGF expression and angiogenesis.6 CJ-42794 blocks pain and inflammation in rat models of arthritis as well as gastric tumorigenesis in mice.7,8 |
| 别名 | RQ-00015986; |
| 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.Takeuchi, K.,Tanaka, A.,Kato, S., et al. Effect of (S)-4-(1-(5-Chloro-2-(4-fluorophenyoxy)benzamido)ethyl) benzoic acid (CJ-42794), a selective antagonist of protaglandin E receptor subtype 4, on ulcerogenic and healing responses in rat gastrointestinal mucosa. Journal of Pharmacology and Experimental Therapeutics 322(3), 903-912 (2007). 5.Murase, A.,Taniguchi, Y.,Tonai-Kachi, H., et al. In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Life Sciences 82(3-4), 226-232 (2008). 6.Hatazawa, R.,Tanaka, A.,Tanigami, M., et al. Cyclooxygenase-2/prostaglandin E2 accelerates the healing of gastric ulcers via EP4 receptors. American Journal of Physiology and Gastrointestinal Liver Physiology 293(4), G788-G797 (2007). 7.Hutamekalin, P.,Takeda, K.,Tani, M., et al. Effect of the C3a-receptor antagonist SB 290157 on anti-OVA polyclonal antibody-induced arthritis. Journal of Pharmacological Sciences 112(1), 56-63 (2010). 8.Oshima, H.,Hioki, K.,Popivanova, B.K., et al. Prostaglandin E2 signaling and bacterial infection recruit tumor-promoting macrophages to mouse gastric tumors. Gastroenterology 140(2), 596-607 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 413.8 |
| 分子式 | C22H17ClFNO4 |
| CAS号 | 847728-01-2 |
| 稳定性 | ≥ 2 years |
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