Formulation: A solid
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
Purity: ≥98%
Formula Markup: C23H15Cl4FN2O3S2
Formula Weight: 592,3
Shelf life (days): 1460
CAS Number: 861238-35-9
Notes: 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}
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