Potent and high affinity P2Y12antagonist (IC50= 11 nM in radioligand competition binding assay, and 25 nM in a GTPγS binding assay). Causes a dose-dependent increase in blood flow and inhibits ADP-induced platelet aggregationin vivo. Antithrombotic.
1.Bach P, Antonsson T, Bylund R, Björkman JA, Österlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F. (2013) Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283.. J Med Chem, 56 (17):(7015-24). [PMID:23899349]
2.Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W et al.. (2014) Structure of the human P2Y12 receptor in complex with an antithrombotic drug.. Nature, 509 (7498):(115-8). [PMID:24670650]
3.Kong D, Xue T, Guo B, Cheng J, Liu S, Wei J, Lu Z, Liu H, Gong G, Lan T et al.. (2019) Optimization of P2Y12 Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties.. J Med Chem, 62 (6):(3088-3106). [PMID:30843696]
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B2216348