107813-86-5

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 (LTD₄; ）.

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 1 J. Med. Chem. 64(22),16512-16529(2021).