Table 1.
EC50 values for activation of Xenopus, mouse, and human PPARs by the fibrate GW2331
| Species | EC50 values, nM
|
||
|---|---|---|---|
| PPARα | PPARγ | PPARβ/δ | |
| Human | 50 | 300 | >1,000 |
| Mouse | 10 | 200 | >1,000 |
| Xenopus | 60 | 360 | 40 |
EC50 values were determined using the GAL4-PPAR chimeras. CV-1 cells were transfected with the various GAL4-PPAR expression plasmids and the cells were treated with GW2331 at concentrations ranging from 1 × 10−10 M to 1 × 10−5 M in 1/3 molar log steps. All data points were tested in triplicate. The overall levels of activation of PPARα and PPARγ were comparable to those obtained with saturating concentrations of Wy 14,643 and BRL 49653, respectively. Similar EC50 values were obtained in two independent experiments.