Lipoprotein lipase (LPL) mediates the hydrolysis of triglycerides in circulating very low density lipoproteins and chylomicrons. NO-1886 is an LPL activator that increases LPL mRNA and LPL activity in adipose tissue, myocardium, and skeletal muscle. This coincides with an elevation in post-heparin plasma LPL activity and LPL mass in rats. NO-1886 decreases plasma triglyceride concentration and increases plasma high-density lipoprotein cholesterol, resulting in inhibited development of atherosclerotic lesions in coronary arteries and aortas of rats and rabbits.