Identification | Back 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 Properties | Back 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 Information | Back 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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