NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research[1].
Biological Activity
NDB is a selective antagonist of human Farnesoid X receptor α (FXRα) th at effectively modulates FXRα down-stream genes.
in vivo
NDB (24 mg/kg; intraperitoneal injection; once a day; for 4 weeks) efficiently decreases the gene expressions of phosphoenolpyruvate carboxykinase (PEPCK), glucose 6-phosphatase (G6-pase), small heterodimer partner, and BSEP in db/db mice[1].
Animal Model:
Male C57BL/6J db/db mice (8 weeks of age)[1]
Dosage:
24 mg/kg
Administration:
Intraperitoneal injection; once a day; for 4 weeks
Result:
Decreased the gene expressions of PEPCK, G6-pase, small heterodimer partner, and BSEP.
References
[1] Xing Xu, et al. Structural Basis for Small Molecule NDB (N-Benzyl-N-(3-(tert-butyl)-4-hydroxyphenyl)-2,6-dichloro-4-(dimethylamino) Benzamide) as a Selective Antagonist of Farnesoid X Receptor α (FXRα) in Stabilizing the Homodimerization of the Receptor. J Biol Chem. 2015 Aug 7;290(32):19888-99. DOI:10.1074/jbc.M114.630475
