CAY10790 is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50 = 2.8 µM) and G protein-coupled bile acid receptor 1 (GPBAR1) agonist.1 It induces receptor transactivation in HEK293T cells expressing human GPBAR1 (EC50 = 3 µM). CAY10790 (10 µM) reduces TNF-α and IL-1β levels in LPS-stimulated RAW 264.7 cells. It also reduces the proliferation of RAW 264.7 cells induced by leukotriene D4 .
1.Fiorillo, B., Sepe, V., Conflitti, P., et al.Structural basis for developing multitarget compounds acting on cysteinyl leukotriene receptor 1 and G-protein-coupled bile acid receptor 1J. Med. Chem.64(22)16512-16529(2021)