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编 号:F095895
分子式:C24H24Cl2N2O2
分子量:443.37
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
AS1708727 is an orally active Foxo1 inhibitor, with EC50 values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively.

体内研究:
AS1708727 (30 to 300 mg/kg, orally) reduces both blood glucose and triglyceride levels, exhibiting anti-diabetic effects.Animal Model:db/db mice aged six weeks.
Dosage:100-1000 mg/kg (Pharmacokinetic Analysis).
Administration:Orally.
Result:Cmax) was 26.7 μM and maximum drug concentration time (Tmax) of 0.5 h at 300 mg/kg.Liver concentration of AS1708727 at 0.5-2 h after oral administration was 3.7- to 5.4-fold higher than the plasma concentration, indicating good liver transition of AS1708727.
Animal Model:Diabetic model mice.
Dosage:30 to 300 mg/kg.
Administration:Orally twice daily for 4 days.
Result:Blood glucose level was significantly reduced at 300 mg/kg.Plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were significantly reduced at 300 mg/kg.G6Pase and PEPCK mRNA levels were significantly reduced at dosages of 100 and 300 mg/kg.

体外研究:
AS1708727 suppresses increases in blood glucose level by inhibiting gluconeogenic gene expression.
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