CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist ( IC 50 =2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist ( EC 50 =3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.