Table 1. Natural and synthetic activators/ligands of PPARβ/δ.
Compound | Comment | Relative affinity for PPARβ/δ* | Reference |
---|---|---|---|
Linoleic acid | Essential dietary fatty acid; also activates PPARα | Micromolar | [165–167] |
Oleic acid | Dietary fatty acid; also activates PPARα and PPARγ | Micromolar | [110,167,168] |
Arachidonic acid | Essential dietary fatty acid; also activates PPARγ | Micromolar | [165] |
Eicosapentaenoic acid | Essential dietary fatty acid; also activates PPARα | Micromolar | [165] |
Docosahexaenoic acid | Essential dietary fatty acid | Micromolar | [165] |
Prostaglandin A1 | Endogenous prostaglandin | Micromolar | [165,169] |
Carbaprostacyclin | Synthetic stable PGI2 analogue; also activates PPARα | Micromolar | [165,169] |
Iliprost | Antihypertensive drug; prostacyclin analogue | Micromolar | [165] |
L165,041 | Synthetic high-affinity ligand; can activate PPARα and PPARγ at high concentration | Nanomolar | [170] |
GW501516 | Synthetic high-affinity ligand; can activate PPARα and PPARγ at high concentration | Nanomolar | [171] |
GW0742 | Synthetic high-affinity ligand; can activate PPARα and PPARγ at high concentration | Nanomolar | [171] |
Relative concentration range required to activate the receptor based on the relative ability to transactivate reporter constructs. PGI2, prostacyclin.