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AS1708727 

Cat. No.: HY-123046
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AS1708727 is an orally active Foxo1 inhibitor, with EC50 values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively.

For research use only. We do not sell to patients.

AS1708727 Chemical Structure

AS1708727 Chemical Structure

CAS No. : 1253226-93-5

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Description

AS1708727 is an orally active Foxo1 inhibitor, with EC50 values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively[1].

In Vitro

AS1708727 suppresses increases in blood glucose level by inhibiting gluconeogenic gene expression[1].

RT-PCR[1]

Cell Line: Fao cells, derived from the H4IIE hepatoma cell line.
Concentration: 0.1-3000 μM.
Incubation Time: 18 h.
Result: Showed dose-dependent reduction in mRNA levels for G6Pase and PEPCK.
In Vivo

AS1708727 (30 to 300 mg/kg, orally) reduces both blood glucose and triglyceride levels, exhibiting anti-diabetic effects[1].

Animal Model: db/db mice aged six weeks[1].
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[1].
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[1].
Animal Model: Diabetic model mice[1].
Dosage: 30 to 300 mg/kg.
Administration: Orally twice daily for 4 days.
Result: Blood glucose level was significantly reduced at 300 mg/kg[1].
Plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were significantly reduced at 300 mg/kg[1].
G6Pase and PEPCK mRNA levels were significantly reduced at dosages of 100 and 300 mg/kg[1].
Molecular Weight

443.37

Formula

C₂₄H₂₄Cl₂N₂O₂

CAS No.

1253226-93-5

SMILES

O=C(CC1CCCC1)N(C)C2=CC=C(C(COC3=CC=CC4=C3C=CN=C4)=C2Cl)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AS1708727AS 1708727AS-1708727Otherstype 2diabetesmellitushypertriglyceridemaiaG6PasePEPCKInhibitorinhibitorinhibit

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AS1708727
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