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1638851-44-1

1638851-44-1 Structure

1638851-44-1 Structure
IdentificationBack Directory
[Name]

HSK 0935)
[CAS]

1638851-44-1
[Synonyms]

HSK 0935)
4R)-Me-Glu
HSK0935 (HSK-0935
HSK0935 (Synonyms: HSK-0935
[Molecular Formula]

C22H25ClO7
[MDL Number]

MFCD31813599
[MOL File]

1638851-44-1.mol
[Molecular Weight]

436.89
Chemical PropertiesBack Directory
[Boiling point ]

597.7±50.0 °C(Predicted)
[density ]

1.43±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

12.54±0.70(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Description]

HSK0935 is a potent and highly selective SGLT2 inhibitors (IC50 (hSGLT2) = 1.3 nM; IC50 (hSGLT1) + 1096nM). HSK0935 demonstrated excellent hSGLT2 inhibition of 1.3 nM and a high hSGLT1/hSGLT2 selectivity of 843-fold. It showed robust urinary glucose excretion in Sprague-Dawley (SD) rats and affected more urinary glucose excretion in Rhesus monkeys.
[Uses]

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

[IC 50]

SGLT2
[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. DOI:10.1021/acs.jmedchem.6b01818
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