A first generation, selective SGLT inhibitor that blocks glucose transport with about 100-fold selectivity for SGLT2 (Ki = 6 nM; EC50 = 1.1 nM) over SGLT1 (Ki = 390 nM); 0.1 to 1.0 mg/kg increases urinary glucose excretion in both normal and diabetic rats, improves glucose tolerance in normal rats, and reduces hyperglycemia in Zucker diabetic fatty rats.