货号 | 13281-10mg |
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 CAY10598 is a very potent agonist of EP4, binding with a Ki value of 1.2 nM.4 Moreover, it does not bind EP1, EP2, EP3, or other prostanoid receptors, including DP, FP, IP, and TP.4 First generation EP4 receptor-selective agonists have been shown to reduce inflammation, improve bone healing, provide cardio- and neuroprotection, and reduce renal dysfunction, suggesting some clinical applications for EP4agonists.5,6,7,8,9 |
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.Billot, X.,Chateauneuf, A.,Chauret, N., et al. Discovery of a potent and selective agonist of the prostaglandin EP4 receptor. Bioorganic & Medicinal Chemistry Letters 13, 1129-1132 (2003). 5.Yamane, H.,Sugimoto, Y.,Tanaka, S., et al. Prostaglandin E2 receptors, EP2 and EP4, differentially modulate TNF-α and IL-6 production induced by lipopolysaccharide in mouse peritoneal neutrophils. Biochemical and Biophysical Research Communications 278, 224-228 (2000). 6.Marui, A.,Hirose, K.,Maruyama, T., et al. Prostaglandin E2EP4 receptor-selective agonist facilitates sternal healing after harvesting bilateral internal thoracic arteries in diabetic rats. J.Thorac.Cardiovasc.Surg. 131(3), 587-593 (2006). 7.Xiao, C.Y.,Yuhki, K.i.,Hara, A., et al. Prostaglandin E2 protects the heart from ischemia-reperfusion injury via its receptor subtype EP4. Circulation 109, 2462-2468 (2004). 8.Ahmad, A.S.,Ahmad, M.,de Brum-Fernandes, A.J., et al. Prostaglandin EP4 receptor agonist protects against acute neurotoxicity. Brain Research 1066, 71-77 (2005). 9.Li, J.H.,Chou, C.L.,Li, B., et al. A selective EP4PGE2 receptor agonist alleviates disease in a new mouse model of X-linked nephrogenic diabetes insipidus. Journal of Clinical Investigation 119(10), 3115-3126 (2009). | |
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 | 383.5 |
分子式 | C21H29N5O2 |
CAS号 | 346673-06-1 |
稳定性 | ≥ 1 year |
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