Description
An EP4 antagonist (IC50s = 0.29 and 0.86 nM for the human and rat receptors, respectively); selective for these receptors over 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); inhibits PGE2-induced increases in cAMP accumulation in Jurkat cells expressing human EP4 and CHO cells expressing the rat receptor (IC50s = 0.29 and 0.86 nM, respectively); inhibits PGE2-induced decreases in LPS-stimulated TNF-α release in isolated rat whole blood; decreases albuminuria in the db/db mouse model of type 2 diabetes at 0.01 and 0.1 mg/kg per day
Formal name: trans-4-[[[[1-(2-quinolinylmethyl)-5-(trifluoromethyl)-1H-indol-7-yl]carbonyl]amino]methyl]-cyclohexanecarboxylic acid
Synonyms:
Molecular weight: 509.5
CAS: 1196045-28-9
Purity: ≥95% (mixture of isomers)
Formulation: A crystalline solid
