This review examines the various effects of Wy14,643, a hypolipidemic agent that activates peroxisome proliferator-activated receptor-α (PPARα), on the cardiovascular system. An emphasis has been placed on the specific cellular processes affected by Wy14,643 as they relate to vascular and cardiac function. Although the topic of this discussion is limited to vascular and cardiac tissues, the importance of circulating lipids on cardiovascular disease requires that a description of the indirect actions of this compound on liver metabolism also be included. Finally, the pharmacology of Wy14,643 is discussed within the context of PPARα-dependent and -independent mechanisms.