Plasma glucose is continuously filtered through the glomerulus in the kidney and then reabsorbed via the transcellular transport systems. Glucose reabsorption in the kidney is mediated by a distinct class of transporters such as sodium-glucose cotransporters (SGLTs). Most of filtered glucose is reabsorbed by the low affinity/high capacity SGLT2 located in the proximal renal tubule. SGLT2 inhibitors, such as T-1095, enhance urinary glucose excretion, and consequently lower blood glucose level and control energy balance in a negative direction. The principle behind SGLT inhibition involves the amelioration of diabetic conditions without increasing body weight or the risk of hypoglycemia. A number of SGLT2 inhibitors are being developed and studies have suggested the therapeutic potential and safety of these drugs for the treatment of diabetes.