Tofogliflozin is a potent inhibitor of sodium glucose cotransporter 2 (SGLT2) with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2, respectively.1 It is selective for SGLT2 (IC50 = 2.9 nM) over other SGLTs (IC50s = >1,500 nM for SGLT1 and 3-6). Tofogliflozin (3-10 mg/kg) reduces plasma glucose concentrations and increases renal glucose clearance in Zucker diabetic fatty rats in a dose-dependent manner. It also reduces hyperglycemia in non-fasted db/db mice and decreases postprandial hyperglycemia in GK rats, a non-obese model of type 2 diabetes with glucose intolerance.
1.Suzuki, M., Honda, K., Fukazawa, M., et al.Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and miceJ. Pharmacol. Exp. Ther.341(3)692-701(2012)