产品描述:
DG-041 is an antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype EP3 (IC50 = 8.1 nM in a calcium mobilization assay).{16959} It is selective for EP3 over DP1, EP1, and TP receptors (IC50s = 131, 486, and 742 nM, respectively, in calcium mobilization assays) as well as EP2, EP4, IP, FP, and DP2/CRTH2 receptors (IC50s = >10,000 nM for all in calcium mobilization assays). DG-041 (1 µM) inhibits collagen- and PGE2-induced platelet aggregation in isolated rat platelets. It inhibits P-selectin expression induced by the TP receptor agonist U-46619 (Item No. 16450) in isolated and washed human platelets when used at a concentration of 3 µM.{20114} DG-041 (10 or 100 mg/kg) inhibits collagen- and PGE2-induced platelet aggregation in rat platelet-rich plasma ex vivo without increasing bleeding time in the same rats.{16959}