| 货号 | 14059-5mg |
| 描述 | The lipid mediator thromboxane A2(TXA2) plays a key role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated by its specific G protein coupled-receptor, referred to as the TXA2 receptor or TP. S18886 is an orally active, long-acting antagonist of the TP receptor with an IC50 value of 16.4 nM.1 It inhibits TP receptor-mediated vascular contractions, platelet aggregation, and adhesion and infiltration of monocytes/macrophages in various pre-clinical and clinical models of thrombosis or atherosclerosis.2,3,4,5 S18886 is the active isomer of the potent TP receptor antagonist, S18204.6 Antagonists of TP receptors have advantages over aspirin (Item No. 70260) as they not only block the effect of TXA2 on platelets, but also inhibit other ligands such as prostaglandin endoperoxides and isoprostanes.5,2 |
| 别名 | Terutroban;Triplion; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wang, X.,Liu, L.,Huang, L., et al. Potent, long-acting cyclopentane-1,3-dione thromboxane (A2)-receptor antagonists. ACS Med.Chem.Lett. 5(9), 1015-1020 (2014). 2.Jones, R.L.,Giembycz, M.A. and Woodward, D.F. Prostanoid receptor antagonists: Development strategies and therapeutic applications. British Journal of Pharmacology 158(1), 104-145 (2009). 3.Hong, T.T.,Huang, J.,Driscoll, E., et al. Preclinical evaluation of S18886 in an experimental model of coronary arterial thrombosis. Journal of Cardiovascular Pharmacology 48(5), 239-248 (2006). 4.Osende, J.I.,Shimbo, D.,Fuster, V., et al. Antithrombotic effects of S 18886, a novel orally active thromboxane A2 receptor antagonist. J.Thromb.Haemost. 2(3), 492-498 (2004). 5.Cayatte, A.J.,Du, Y.,Oliver-Krasinski, J., et al. The thromboxane receptor antagonist S18886 but not aspirin inhibits atherogenesis in apo E-deficient mice: Evidence that eicosanoids other than thromboxane contribute to atherosclerosis. Artioscler.Thromb.Vasc.Biol. 20(7), 1724-1728 (2000). 6.Simonet, S.,Descombes, J.J.,Vallez, M.O., et al. S 18886, a new thromboxane (TP)-receptor antagonist is the active isomer of S 18204 in all species, except in the guinea-pig. Advances in Experimental Medicine and Biology 433, 173-176 (1997). | |
| 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 | 407.9 |
| 分子式 | C20H22ClNO4S |
| CAS号 | 165538-40-9 |
| 稳定性 | ≥ 2 years |
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