Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.
Fexaramine 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Wild-type C57BL/6J mice and db/db mice
Oral gavage
50 mg/kg
Once a day for 7 to 9 days
FEX markedly increased taurolithocholic acid (TLCA), increased fibroblast growth factor 15 (FGF15) and FGF21 and GLP-1 secretion, improved insulin and glucose tolerance, and promoted white adipose tissue browning in mice.
Hepatology. 2018 Oct;68(4):1574-1588
C57BL/6 mice
Alcoholic liver disease model
Oral gavage
100mg/kg BW
Daily for 8 weeks
To evaluate the protective effect of Fexaramine on alcoholic liver disease. Results showed that Fexaramine reduced ethanol-induced liver injury and steatosis, decreased hepatic inflammatory markers IL1B and TNF protein expression, and stabilized gut barrier function.
Hepatology. 2018 Jun;67(6):2150-2166
Mice
High-fat diet-induced metabolic syndrome model
Gavage
100 mg/kg/day
Once daily for 6 weeks
To evaluate whether Fexaramine affects the amelioration of metabolic syndrome by reversing the inhibitory effect of tryptophan on intestinal FXR signaling. Results showed that Fexaramine reversed the Trp-induced reduction in FGF15 protein levels and the Trp-induced increase in BA levels.
Research (Wash D C). 2024 Dec 13;7:0515
Mice
High-fat diet-induced NASH model
Dietary administration
50 mg/kg body weight/day
Daily administration for 3 weeks
Evaluate the effect of Fexaramine on NASH and metabolic disorders. Results showed that Fexaramine did not significantly increase FXR activation, did not raise TGR5 ligands, did not modulate TGR5 signaling, and did not regulate GLP-1 secretion.
Nutrients. 2022 Jun 29;14(13):2707
Mice
High-fat diet-induced obesity model
Oral gavage
50 mg or 100 mg/kg body weight
Once daily for 5 weeks
Fexaramine reduces diet-induced weight gain and metabolic syndrome by promoting energy expenditure and browning of white adipose tissue.
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