Tofogliflozin (hydrate)  (Synonyms: CSG-452 hydrate)

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: 2.9 nM (SGLT2); Ki: 2.9 nM ( human SGLT2), 14.9 nM (rat SGLT2), and 6.4 nM (mouse SGLT2)^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

404.45

Solid

C₂₂H₂₈O₇

1201913-82-7

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Room temperature in continental US; may vary elsewhere.

• [1]. Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701.  [Content Brief]

  [2]. Ishibashi Y, et al. Tofogliflozin, A Highly Selective Inhibitor of SGLT2 Blocks Proinflammatory and Proapoptotic Effects of Glucose Overload on Proximal Tubular Cells Partly by Suppressing Oxidative Stress Generation. Horm Metab Res. 2016 Mar;48(3):191-5.  [Content Brief]