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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[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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