Elafibranor (also known as GFT-505) is a dual PPARα/δ agonist with EC50s of 45 and 175 nM, respectively. Elafibranor (GFT505) treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with Elafibranor.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male db/db and db/lean mice |
| Formulation | 0.1% Tween 80 and 1% carboxymethylcellulose in 98.9% distilled water |
| Dosages | 3, 10 and 30 mg/kg/day |
| Administration | oral gavage |
| Molecular Weight | 384.49 |
| Formula | C22H24O4S |
| CAS Number | 923978-27-2 |
| Solubility (25°C) | DMSO ≥ 33 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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|---|
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DSO-5a is a potent, selective, orally active BB3 agonist. |
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| 3-Phenyl-2-propen-1-ol
trans-Cinnamyl alcohol is a trans-isomer of Cinnamyl alcohol. |
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