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.
IC50&Target
IC50: 40 μM (FXR)
体外研究
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.
体内研究
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.
Animal Model:
APCmin/+ mice
Dosage:
400 mg/kg
Administration:
Oral gavage; twice a week; for 6 weeks
Result:
Markedly decreased intestinal integrity and accelerated tumor growth in the intestine and colon.
分子式
C26H44NNaO7S
分子量
537.68
CAS号
145022-92-0
运输条件
Room temperature in continental US; may vary elsewhere.