Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC₅₀ of 2.9 nM and K_i values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2^[1]. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells^[2]. IC50 & Target: IC50: 2.9 nM (SGLT2); Ki: 2.9 nM ( human SGLT2), 14.9 nM (rat SGLT2), and 6.4 nM (mouse SGLT2)^[1] In Vitro: Tofofloxacin (3-30 nM; 24 hours; tubular epithelial cells) treatment inhibits the oxidative stress generation and monocyte chemoattractant protein-1 (MCP-1) gene expression in tubular cells induced by high glucose^[2].
Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose^[2]. In Vivo: Tofogliflozin (0.1-10 mg/kg; oral administration; once daily; for 4 weeks; db/db mice) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice^[1].