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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.
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| Cell lines | |
| Preparation method | |
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| Animal Experiment | |
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| 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 |
| Related PPAR Products |
|---|
| GQ-16
GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. |
| SR10221
SR10221, a noncovalent inverse agonist of PPARγ, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines. |
| Amorfrutin B
Amorfrutin B is a highly potent natural peroxisome proliferation-activated receptor γ (PPARγ) agonist with oral activity with Ki values of 19 nM and EC50 values of 73 nM, respectively. |
| Netoglitazone
Netoglitazone is a dual agonist of PPARα and PPARγ with antihyperglycemic activity. |
| DSO-5a
DSO-5a is a potent, selective, orally active BB3 agonist. |
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