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. Author manuscript; available in PMC: 2009 Aug 1.
Published in final edited form as: Clin Sci (Lond). 2008 Aug;115(4):107–127. doi: 10.1042/CS20080022

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.