DG-041

DG-041 is an antagonist of the prostaglandin E2 (PGE2, Cay-14010) receptor subtype EP3 (IC50 = 8.1 nM in a calcium mobilization assay). 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 (Cay-16450) in isolated and washed human platelets when used at a concentration of 3 µM. 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.Formal Name: (2E)-3-[1-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-1H-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide. CAS Number: 861238-35-9. Molecular Formula: C23H15Cl4FN2O3S2. Formula Weight: 592.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml. SMILES: CC1=CN(CC2=C(Cl)C=C(Cl)C=C2)C3=C1C=C(F)C=C3/C=C/C(NS(C4=CC(Cl)=C(Cl)S4)(=O)=O)=O. InChi Code: InChI=1S/C23H15Cl4FN2O3S2/c1-12-10-30(11-14-2-4-15(24)7-18(14)25)22-13(6-16(28)8-17(12)22)3-5-20(31)29-35(32,33)21-9-19(26)23(27)34-21/h2-10H,11H2,1H3,(H,29,31)/b5-3+. InChi Key: BFBTVZNKWXWKNZ-HWKANZROSA-N.