NDB is a selectivehuman FXRα (hFXRα)antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research^[1].

Human FXRα (hFXRα)^[1]

NDB induces rearrangements of helix 11 (H11) and helix 12 (H12, AF-2) by forming a homodimer of hFXRα-LBD, totally different from the active conformation in monomer state^[1].
NDB (25 μM) effectively antagonizes the GW4064-stimulated FXR/RXR interaction and FXRα target gene expression in primary mouse hepatocytes, including the small heterodimer partner (SHP) and bile-salt export pump (BSEP)^[1].

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].

471.42

C₂₆H₂₈Cl₂N₂O₂

1660153-08-1

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