ASP7657

ASP7657 is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 (Kis = 2.21 and 6.02 nM for the human and rat receptors, respectively). It is selective for these receptors over the rat EP1, EP2, and EP3 receptors (IC50s = >1,000 nM for all), as well as a panel of 42 additional receptors and ion channels (IC50s = >1,000 nM for all). ASP7657 inhibits increases in cAMP accumulation induced by PGE2 in Jurkat cells expressing human EP4 and CHO cells expressing the rat receptor with IC50 values of 0.29 and 0.86 nM, respectively. It inhibits PGE2-induced decreases in LPS-stimulated TNF-alpha release in isolated rat whole blood in a dose-dependent manner. AP7657 (0.01 and 0.1 mg/kg per day) decreases albuminuria in the db/db mouse model of type 2 diabetes.Formal Name: trans-4-[[[[1-(2-quinolinylmethyl)-5-(trifluoromethyl)-1H-indol-7-yl]carbonyl]amino]methyl]-cyclohexanecarboxylic acid. CAS Number: 1196045-28-9. Molecular Formula: C28H26F3N3O3. Formula Weight: 509.5. Purity: >95% (mixture of isomers). Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16.5mg/mL, DMSO: 16.5mg/mL, DMSO:PBS (pH 7.2) (1:3): 0.25mg/mL, Ethanol: 12.5mg/mL. lambdamax: 234 nm. SMILES: OC([C@H]1CC[C@H](CNC(C2=C(N(CC3=NC(C=CC=C4)=C4C=C3)C=C5)C5=CC(C(F)(F)F)=C2)=O)CC1)=O. InChi Code: InChI=1S/C28H26F3N3O3/c29-28(30,31)21-13-20-11-12-34(16-22-10-9-18-3-1-2-4-24(18)33-22)25(20)23(14-21)26(35)32-15-17-5-7-19(8-6-17)27(36)37/h1-4,9-14,17,19H,5-8,15-16H2,(H,32,35)(H,36,37)/t17-,19-. InChi Key: HBDTYYZZYCVTIJ-UAPYVXQJSA-N.