| Bioactivity | HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities[1]. | |||||||||
| Target | IC50: 1.3 nM (SGLT2) | |||||||||
| Invitro | HSK0935 (Compound 31) demonstrates excellent hSGLT2 inhibition of 1.3 nM and a high hSGLT1/hSGLT2 selectivity of 843-fold[1]. | |||||||||
| In Vivo | 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]. | |||||||||
| Name | HSK0935 | |||||||||
| CAS | 1638851-44-1 | |||||||||
| Formula | C22H25ClO7 | |||||||||
| Molar Mass | 436.88 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. |