Abstract: Sodium-dependent glucose transporters 2 mainly found in the S1 segment of the proximal tubule of the nephron is a low-affinity, high-capacity transporter believed to account for 90% of the renal glucose reabsorption. Therefore, inhibiting the activity of SGLT2, blocking this reabsoption and increasing the amount of glucose excretion, has been proposed as a novel strategy for treating diabetes. The latest research progress on SGLT2 inhibitors was introduced. Additionally, Canagliflozin, the first SGLT2 inhibitor approved by FDA was described in detail, including its synthesis, pharmacokinetics, pharmacodynamics, clinical research and adverse effects and so on.