Tofogliflozin hydrate

Tofogliflozin (CSG-452) is a potent, highly selective SGLT2 inhibitor with Ki of 2.9, 14.9, and 6.4 nM against human, rat, and mouse SGLT2, respectively; displays high selectivity over human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1; increases renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats, also improves postprandial glucose excursion; reduces glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test in vivo.Diabetes Approved (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.Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose. (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.