| Identification | Back Directory | [Name]
Cyclopentaneacetamide, N-[2,4-dichloro-3-[(5-isoquinolinyloxy)methyl]phenyl]-N-methyl- | [CAS]
1253226-93-5 | [Synonyms]
AS1708727
Cyclopentaneacetamide, N-[2,4-dichloro-3-[(5-isoquinolinyloxy)methyl]phenyl]-N-methyl- | [Molecular Formula]
C24H24Cl2N2O2 | [MDL Number]
MFCD30186588 | [MOL File]
1253226-93-5.mol | [Molecular Weight]
443.37 |
| Hazard Information | Back Directory | [Uses]
AS1708727 is an orally active Foxo1 inhibitor, with EC50 values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively[1]. | [Biological Activity]
AS1708727 is an orally active Foxo1 inhibitor, with EC50 values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively[1].
AS1708727 suppresses increases in blood glucose level by inhibiting gluconeogenic gene expression[1].
AS1708727 (30 to 300 mg/kg, orally) reduces both blood glucose and triglyceride levels, exhibiting anti-diabetic effects[1]. | [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].
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| 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].
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| [storage]
Store at -20°C | [References]
[1]. Hirotsugu Tanaka, et al. Effects of the Novel Foxo1 Inhibitor AS1708727 on Plasma Glucose and Triglyceride Levels in Diabetic Db/Db Mice. Eur J Pharmacol. 2010 Oct 25;645(1-3):185-91. |
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