Ipragliflozin (L-Proline)

Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC₅₀ of 2.8 nM; little and NO potency for SGLT1/3/4/5/6. IC50 & Target: IC50 value: 2.8 nM (SGLT2)^[1][2]. In Vitro: Ipragliflozin (L-Proline) potently and selectively inhibits human, rat, and mouse SGLT2 at nanomolar ranges and exhibits stability against intestinal glucosidases^[3]. In Vivo: Ipragliflozin (L-Proline) shows good pharmacokinetic properties following oral dosing, and dose-dependently increases urinary glucose excretion, which lasts for over 12 h in normal mice ^[3]. Oral administration of ipragliflozin increases urinary glucose excretion in a dose-dependent manner, an effect which is significant at doses of 0.3 mg/kg or higher and lasts over 12 h^[4]. Single administration of ipragliflozin dose-dependently increases urinary glucose excretion, reduces blood glucose and plasma insulin levels, and improves glucose intolerance ^[5].