Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM[2].IC50 & Target:IC50: 40 μM (FXR)In Vitro: T-βMCA sodium inhibits FXR reporter activity in the CRC cell line HT29 (EC50 ~10 μM).
T-βMCA sodium dose-dependently increases WNT signaling in HT29 and HCT116 cells.
T-βMCA sodium induces proliferation and DNA damage in Lgr5+ cells.
In Vivo: T-βMCA sodium (400 mg/kg; i.g.; twice a week; for 6 weeks) can effectively recapitulate the ability of HFD to promote CRC progression.
T-βMCA sodium treatment also significantly increases levels of serum cytokines, including IFN-γ, IL-6, and IL-17.