Table 2.
Influence of the CysLT1RA on the activation of PPAR reporter constructs.
| PPARα | PPARγ | PPARδ | CysLT1R | |
|---|---|---|---|---|
| EC50 [μM] | IC50 [nM] | |||
| Zafirlukast | i.a. @ 10 μM | 2.49 ± 0.45 μM (148 ± 15%) | i.a. @ 10 μM | 5 |
| Montelukast | i.a. @ 10 μM | 1.17 ± 0.08 μM (21.9 ± 0.3%) | i.a. @ 10 μM | 5 |
| Pranlukast | i.a. @ 10 μM | @ 10 μM (19.7 ± 1.1%) | i.a. @ 10 μM | 4 |
Employing reporter gene assays for the respective PPAR isoforms, EC50 values of the CysLT1RA were determined in HEK-293T cells. PPAR activation of the positive controls GW-7647 (PPARα), pioglitazone (PPARγ) and L165,041 (PPARδ) were set to 100% and receptor activation of the CysLT1RAs were calculated accordingly. Results are shown as ±SEM of three independent experiments. i.a., inactive.