IC50: 1.3 nM (SGLT2)[1]
HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antiperglycemic activities[1].
HSK0935 (Compound 31) demonstrates excellent hSGLT2 inhibition of 1.3 nM and a high hSGLT1/hSGLT2 selectivity of 843-fold[1].
HSK0935 treatment (1, 3, and 10 mg/kg) shows robust urinary glucose excretion in Sprague-Dawley (SD) rats and affects more urinary glucose excretion in Rhesus monkeys[1].
HSK0935 is well tolerated up to 300 mg/kg without any mortality or severe untoward effects in a 28-day repeat-dose toxicology study in beagle dogs[1].
[1]. Li Y, et al. Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes. J Med Chem. 2017 May 25;60(10):4173-4184.