HSK0935

Names

[ Name ]:
HSK0935

Biological Activity

[Description]:

HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities[1].

[Related Catalog]:

Research Areas >> Metabolic Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> SGLT

[Target]

IC50: 1.3 nM (SGLT2)[1]

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₅ClO₇

[ Molecular Weight ]:
436.88

HSK0935

Names

Biological Activity

Chemical & Physical Properties

Related Compounds