Abstract Renalase, a novel amine oxidase, is mainly expressed in the kidney, heart, and skeletal muscle. It has been known to degrade circulating catecholamines and plays a crucial role in human diseases. Recent studies have demonstrated its structure, unique bioactivities, function, and the gene polymorphisms in human diseases. In this review, we summarize the effects of renalase on hypertension, myocardial ischemia, acute kidney injury (AKI), ischemic stroke, cardiac dysfunction, organ transplantation, and diabetes mellitus reported in numerous studies.