Table 1.
Transactivation assays in COS-7 cells
| Gal4-PPARα (LBD) | Gal4-PPARγ (LBD) | Gal4-PPARδ (LBD) | ||||
|---|---|---|---|---|---|---|
| EC50 (μM) | TOP (% ref) | EC50 (μM) | TOP (% ref) | EC50 (μM) | TOP (% ref) | |
| Murine | 0.02 | 78 | 0.01 | 65 | 0.01 | 84 |
| Human | 0.03 | 57 | 0.06 | 61 | 0.07 | 84 |
Transactivation assays were performed in COS-7 cells. The Emax effect of GFT1803 is calculated relative to the maximal induction obtained with the corresponding reference compound in the same experiment. The reference compounds for PPARα, PPARγ, and PPARδ were fenofibrate (100 μM), rosiglitazone (10 μM), and GW501516 (1 μM), respectively