WAY-362450 (Turofexorate isopropyl; XL335) is a synthetic potent agonists of the farnesoid X receptor (FXR). WAY-362450 binds to the ligand-binding domain (LBD) of human FXR. WAY-362450 (XL335) also induced small heterodimer partner (SHP) expression and repressed cholesterol 7alpha-hydroxylase (CYP7A1) and sterol 12 alpha-hydroxylase (CYP8B1) expression. Oral administration of WAY-362450 to LDLR(-/-) mice results in lowering of cholesterol and triglycerides. Furthermore, treatment of wild type C57BL/6 mice with the FXR agonist WAY-362450, attenuated lipopolysaccharide-induced serum amyloid P component and serum amyloid A3 mRNA levels in the liver.
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Source | Biochem Biophys Res Commun (2014). Figure 1. WAY-362450 |
| Method | qRT-PCR | |
| Cell Lines | Huh7 cells | |
| Concentrations | 3 μM | |
| Incubation Time | 24 h | |
| Results | No significant pathological changes were found and liver lipid staining is minimal in control liver specimens. Feeding 30% fructose for 8 weeks led to a nearly 6-fold increase of lipids contents in serum and liver respectively, and induced significant hepatic steatosis, characterized by the presence of macrovesicular and microvesicular lipid droplets in hepatocytes. |
| Molecular Weight | 438.47 |
| Formula | C25H24F2N2O3 |
| CAS Number | 629664-81-9 |
| Solubility (25°C) | DMSO 25 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.
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