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DG 041 是一种有效的、高亲和力和选择性的 EP3 受体拮抗剂,在结合和 FLIPR 试验中的 IC50 分别为 4.6 nM 和 8.1 nM。
Potent and selective EP3 antagonist (IC50 = 4.6 nM). Inhibits PGE2 facilitation of platelet aggregation in vitro and ex vivo. Displays good plasma and metabolic stability. Does not affect bleeding time in rats. Antiplatelet and antithrombotic.
Markovi? et al (2017) Structural features of subtype-selective EP receptor modulators. Drug Discov.Today. 22 57 PMID:27506873 |Singh et al (2009) Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding. ACS Chem.Biol. 4 115 PMID:19193156
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