Molecular Formula | C18H22FN3O3 |
Molar Mass | 347.38 |
Density | 1.370±0.06 g/cm3(Predicted) |
Boling Point | 587.3±50.0 °C(Predicted) |
Solubility | DMSO: 7.6 mg/mL (Need ultrasonic and warming) |
pKa | 6.47±0.50(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
In vitro study | AS1842856 inhibits foxo1-mediated transactivation by direct binding to foxo1. In HepG2 cells Transiently transfected with the Foxo1 expression vector, AS1842856 effectively inhibited foxo1-mediated promoter activity, a dose-dependent effect similar to that of insulin treatment. 0.1 μm AS1842856 inhibited 3% Foxo3a-and 20% Foxo4-mediated promoter activity, respectively. In contrast, foxo1-mediated promoter activity was reduced by 70%. Foxo1 inhibitor AS1842856 may inhibit the activity of endogenous G6Pase and PEPCK by reducing the mRNA levels of G6Pase and PEPCK, which may inhibit the production of glucose in Fao cells. |
In vivo study | Oral administration of AS1842856 to db/db mutant mice with diabetes resulted in a significant decrease in fasting blood glucose by inhibiting liver gluconeogenesis-related genes. Normal mice after oral administration of AS1842856 has no such effect. Treatment with AS1842856 also inhibited the rise in blood glucose levels caused by injection of pyruvate (normal mice and db/db mice). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.879 ml | 14.393 ml | 28.787 ml |
5 mM | 0.576 ml | 2.879 ml | 5.757 ml |
10 mM | 0.288 ml | 1.439 ml | 2.879 ml |
5 mM | 0.058 ml | 0.288 ml | 0.576 ml |
biological activity | AS1842856 is a cell permeable inhibitor that inhibits the transcriptional activity of Foxo1 with IC50 = 33 nM. AS1842856 binds directly to activated Foxo1, but does not bind to Foxo1 phosphorylated at ser256. AS1842856 can inhibit autophagy. |
Target | TargetValue Foxo1 (In HepG2 cells) 33nM |
Target | Value |
Foxo1 (In HepG2 cells) | 33nM |
in vitro study | AS1842856 inhibits foxo1-mediated transactivation by direct binding to foxo1. In HepG2 cells Transiently transfected with the Foxo1 expression vector, AS1842856 effectively inhibited foxo1-mediated promoter activity, a dose-dependent effect similar to that of insulin treatment. 0.1 μm AS1842856 inhibited 3% Foxo3a-and 20% Foxo4-mediated promoter activity, respectively. In contrast, foxo1-mediated promoter activity was reduced by 70%. Foxo1 inhibitor AS1842856 may inhibit the activity of endogenous G6Pase and PEPCK by reducing the mRNA levels of G6Pase and PEPCK, which may inhibit the production of glucose in Fao cells. |
in vivo study | The db/db mutant mice with diabetes mellitus were orally administered with AS1842856, through inhibition of liver gluconeogenesis-related genes, resulting in a significant decline in their fasting blood glucose values. Normal mice after oral administration of AS1842856 has no such effect. Treatment with AS1842856 also inhibited the rise in blood glucose levels caused by injection of pyruvate (normal mice and db/db mice). |