Glucose is the primary energy fuel of life. A glucose transporter, the sodium–glucose transporter (SGLT), is receiving attention as a novel therapeutic target in disease. This review summarizes the physiological role of SGLT in cerebral ischemia, cancer, cardiac disease, and intestinal ischemia, which has encouraged analysis of SGLT function. In cerebral ischemia and cardiomyopathy, SGLT-1 is involved in worsening of the injury. In addition, SGLT-1 promotes the development of cancer. On the other hand, SGLT-1 has a protective effect against cardiac and intestinal ischemia. Interestingly, SGLT-1 expression levels are increased in some diseased tissue, such as in cerebral ischemia and cancer. This suggests that SGLT-1 may have an important role in many diseases. This review discusses the potential of SGLT as a target for novel therapeutic agents.