G protein-coupled receptor 5 (TGR5) is recently discovered to be a new membrane receptor that can regulate inflammation and metabolism. TGR5 activation can inhibit foam cell formation and atherosclerotic plaque rupture by reducing inflammation reaction, promote NO, H₂S and other endogenous gas signal molecules to improve vascular endothelial dysfunction. In addition, it also can reduce atherosclerosis risk factors such as obesity and diabetes. Therefore, TGR5 may be an important target for prevention and treatment of atherosclerosis.