产品
编 号:F746594
分子式:C26H28Cl2N2O2
分子量:471.42
产品类型
结构图
CAS No: 1660153-08-1
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产品详情
生物活性:
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.
体内研究:
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.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.
体外研究:
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).