货号 | 19023-25mg |
描述 | Thromboxane (TXA2) activates the T prostanoid (TP) receptor. Prostaglandin E2(PGE2) activates four E prostanoid (EP) receptors, EP1-4. AH-23848 is a dual antagonist of TP1 and EP4receptors.2 It originally was found to inhibit TXA2-induced platelet aggregation (IC50 = 0.26 μM)1 and the contraction of human bronchial smooth muscle induced by the TP agonist U-46619.3 AH-23848 was subsequently demonstrated to impair PGE2-mediated relaxation of piglet saphenous vein by antagonizing the PGE2 receptor EP4.2 By inhibiting EP4, it likewise suppresses serum-induced cAMP generation, cyclin A synthesis, and the proliferation of fibroblasts4, as well as reduces metastasis in a mouse model of metastatic breast cancer.5 |
供应商 | Cayman |
应用文献 | |
1.Brittain, R.T.,Boutal, L.,Carter, M.C., et al. AH23848: A thromboxane receptor-blocking drug that can clarify the pathophysiologic role of thromboxane A2. Circulation 72, 1208-1218 (1985). 2.Coleman, R.A.,Grix, S.P.,Head, S.A., et al. A novel inhibitory prostanoid receptor in piglet saphenous vein. Prostaglandins 47, 151-168 (1994). 3.Coleman, R.A. and Sheldrick, R.L.G. Prostanoid-induced contraction of human bronchial smooth muscle is mediated by TP-receptors. British Journal of Pharmacology 96, 688-692 (1989). 4.Sanchez, T. and Moreno, J.J. Role of EP1 and EP4PGE2 subtype receptors in serum-induced 3T6 fibroblast cycle progression and proliferation. American Journal of Physiology.Cell Physiology 282, C280-C288 (2002). 5.Ma, X.,Kundu, N.,Rifat, S., et al. Prostaglandin E receptor EP4 antagonism inhibits breast cancer metastasis. Cancer Research 66(6), 2923-2927 (2006). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥90% |
计算分子量 | 496.6 |
分子式 | C29H34NO5 • 1/2Ca |
CAS号 | 81496-19-7 |
稳定性 | ≥ 2 years |
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