Japanese scientists discovered AdipoRon during screening of a compound library. This drug is a selective agonist of adiponectin receptors 1 and 2, which activates 5′-adenosine monophosphate–activated protein kinase (AMPK) in cultured mammalian cells, an enzyme that is involved in many metabolic processes including the release of insulin, inhibition of lipid synthesis, and stimulation of glucose uptake. It was found, that after oral administration in mice AdipoRon effectively attenuated post-ischemic cardiac injury, thus could be a promising novel therapeutic approach treating cardiovascular complications caused by obesity-related disorders such as type 2 diabetes. In addition, recently investigation showed that AdipoRon has antiproliferative effects of adiponectin and may suppress the colorectal cancer cell growth.