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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
[3] S Magotteaux, et al. Marfan syndrome in childhood and adolescence
[4] Kaleb Michaud. The National Data Bank for Rheumatic Diseases (NDB)
| Related Farnesoid X Receptor Products |
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| WAY-362450 (Turofexorate isopropyl)
WAY-362450 (Turofexorate isopropyl; XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM. |
| Chenodeoxycholic acid
Chenodeoxycholic acid is an epimer of ursodeoxycholic acid, which inhibits the production of cholesterol in the liver and absorption in the intestines. |
| Obeticholic Acid (INT-747)
Obeticholic Acid (INT-747) is a potent, orally active, selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.May be used in studies related to non-alcoholic steatohepatitis (NASH). |
| Sevelamer HCl
Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption. |
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