NDB

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 In Vitro 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. 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J db/db mice (8 weeks of age) 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. Form:Solid IC50& Target:Human FXRα (hFXRα)

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