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Characteristics of SR10171 and rosiglitazone.
| Compound | IC50 (nM)a PPARγ | EC50 (nM) PPARγ GAL-4 | EC50 (nM) PPARγ PPRE | % inhibition S273pPPARγ (20 μM) | IC50 (μM)a PPARα | EC50 (μM) PPARα GAL-4 |
|---|---|---|---|---|---|---|
| Rosiglitazone | 18 | 7.4 (100%) | 10 | 100 | No binding | No activity |
| SR10171 | 220 | 7260 (4%) | Inverse agonist | 54 | 1.1 | 1.5 |
LanthaScreen; IC50 — half maximal inhibitory concentration; EC50 — half maximal effective concentration.
