S18886

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

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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. Br. J. Pharmacol. 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. J. Biomed. Sci. 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. Adv. Exp. Med. Biol. 433, 173-176 (1997).