LY3127760 is a potent, selective prostaglandin E4 (EP4) receptor antagonist with binding Ki of 58 nM (hEP4) and cAMP IC50 of 5.6 nM.
LY3127760 shows exquisite selectivity over other EP receptors, with no detectable binding for EP1, EP2 or EP3.
LY3127760 displays an IC50 of 123 nM for inhibition of PGE2-induced TNFa reduction in an ex vivo LPS-stimulated human whole blood assay, a >10-fold increase in potency over CJ023,423 (Cat. PC-42700) in the same assay.
LY3127760 is active in the rat EP4 functional assay (rEP4 IC50 = 12 nM) and a suitable candidate for study in animal models of pain and inflammation.
LY3127760 (30 mg/kg) blocks inflammation in the rat adjuvant induced arthritis (AIA) model.
