Fexaramine

Fexaramine is a potent and selective FXR agonist with an EC₅₀ of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors^[1][2]. In Vitro: Bile acid treatment is performed in HuTu-80 cells with Fexaramine (5, 25, and 50 μM) for 24 h. Fexaramine (50 μM) increases small heterodimer partner (SHP) transcript levels by 2.1-fold. The cells are treated with various concentrations of Fexaramine, and the endogenous secretin transcript levels are significantly reduced (33% in 50 μM Fexaramine). Fexaramine treatment also significantly suppresses secretin promoter activity by 32%^[1]. In Vivo: Fexaramine treatment of DIO mice produces a striking metabolic profile that includes reduced weight gain, decreased inflammation, browning of WAT and increased insulin sensitization^[3].