GW7647 is a potent agonist of PPARα (EC50s: 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ, and PPARδ, respectively).

GW7647 at a concentration of 50 nM, promotes PI3K and Akt (Ser473) phosphorylation, leading to an increase in NOS1 phosphorylation and subsequently elevating NO levels in stripped antral mucosa. Additionally, at the same concentration, it boosts the initial phase of Ca2+-mediated exocytotic events triggered by ACh in antral mucous cells, without independently inducing any exocytotic events. At a higher concentration of 1 μM, GW7647 substantially elevates PDZK1 protein levels to 129.7 ± 6.5% compared to controls in Caco2BBE cells, irrespective of IL-1β presence, and mitigates the IL-1β-induced reduction in PDZK1 expression. When combined with ACh, GW7647 augments the impact of wortmannin (50 nM) and AKT-inh (100 nM) on exocytotic activity in these cells. At 100 nM, GW7647 significantly decreases AQP9 protein levels by 43% in WIF-B9 hepatocytes and by 24% in HepG2 cells, though it shows no notable effects at 10 and 1,000 nM in WIF-B9 hepatocytes, nor does it significantly affect L-FABP protein levels in HepG2 hepatocytes.

GW7647 (3 mg/kg per day) does not avoid the development of cardiac hypertrophy. It prevents the decline in left ventricular ejection fraction in vivo[4].