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Potency and selectivity of GW501516, 5a, and 5b for human PPARs.
| Compounds | Potency (EC50 , nM) | Selectivity index* | |||
|---|---|---|---|---|---|
| hPPARα | hPPARδ | hPPARγ | hPPARα/hPPARδ | hPPARγ/hPPARδ | |
| GW501516 | 300 | 1.2 | 1200 | 250 | 1000 |
| 5a | >10000 | 0.7 | >10000 | >14000 | >14000 |
| 5b | >10000 | 4.3 | >10000 | >2300 | >2300 |
* Selectivity index represents the selectivity for the PPARδ isoform and is given as the ratio of EC50(hPPARα)/EC50(hPPARδ) or EC50(hPPARγ)/EC50(hPPARδ).
EC50: half maximal effective concentration; nd: not determined.
