Dapagliflozin
Dapagliflozin is an inhibitor of sodium-glucose transporter 2 (SGLT2; IC50s = 1.12 and 3 nM for the human and rat enzymes, respectively).{22762} It is selective for SGLT2 over SGLT1 (IC50s = 1,391 and 620 nM for the human and rat enzymes, respectively) and human adipocyte glucose transporter (GLUT) activity at 20 µM. Dapagliflozin (0.1 and 1 mg/kg) increases urinary glucose levels in normal and Zucker diabetic rats. It decreases fasting and fed plasma glucose levels in Zucker diabetic rats when administered at doses of 0.01, 0.1, and 1 mg/kg.
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