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).
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Source | PLoS One (2013). Figure 3. INT-747 |
| Method | H&E staining | |
| Cell Lines | Dahl salt-sensitive (SS/JrHsd) male | |
| Concentrations | 10 mg/kg/day | |
| Incubation Time | 6 weeks | |
| Results | Furthermore, INT-747 did not improve renal pathology in the HS-fed animals. In all HS animals, severe thrombotic microangiopathy (TMA) was observed as well as fibrinoid necrosis of afferent arterioles with an onion-skin pattern of periarterial fibrosis and extravasation of erythrocytes |
| Molecular Weight | 420.63 |
| Formula | C26H44O4 |
| CAS Number | 459789-99-2 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[2] Fiorucci S, et al. Expert Opin Ther Targets. Targeting FXR in cholestasis: hype or hope.
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