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NDB is a selective antagonist of human Farnesoid X receptor α (FXRα) that effectively modulates FXRα down-stream genes.
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).
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.
Molecular Weight | 471.42 |
Formula | C26H28Cl2N2O2 |
CAS Number | 1660153-08-1 |
Form | Solid |
Solubility (25°C) | DMSO 90 mg/mL |
Storage | Powder -20°C |
[1] Lee Crosby, et al. Ketogenic Diets and Chronic Disease: Weighing the Benefits Against the Risks
[2] Paola Caruso, et al. Focus on neuro-Behçet's disease: A review
[4] S Magotteaux, et al. Marfan syndrome in childhood and adolescence
[5] Kaleb Michaud. The National Data Bank for Rheumatic Diseases (NDB)
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