FBPase-IN-7
FBPase-IN-7 is a fructose-1,6-bisphosphatase (FBPase) inhibitor with an IC50 of 0.75 μM. FBPase-IN-7 binds to a cryptic allosteric pocket of FBPase, induces conformational rearrangement of key residues, forms a hydrogen-bond network, and disrupts substrate catalysis. FBPase-IN-7 confirms cellular stabilizes HuFBPase in hepatic cells. FBPase-IN-7 has hypoglycemic activity. FBPase-IN-7 can be used for the research of type 2 diabetes.
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- Formule: C23H15F2N3O6S2
- Masse moléculaire:531.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
FBPase-IN-7 (Compound 29) potently inhibits purified human fructose-1,6-bisphosphatase (FBPase) with an IC50 of 0.75 μM[1].
FBPase-IN-7 (20 μM) directly engages HuFBPase in LO2 human liver cells, conferring a thermal stabilization[1].
FBPase-IN-7 (24 h) shows minimal cytotoxicity in LO2 human liver cells and HEK293T human embryonic kidney cells, with EC50 values >50 μM for both cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice with glucose challenge (2 g/kg) (male, 20-24 g, 12 h-fasted, oral glucose tolerance test model)[1]
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Dosage:100 mg/kg
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Administration:i.p.; single dose
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Result:Reduced the blood glucose AUC0-1.5ₕ by 20.6%.
Chemical Information
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Masse moléculaire 531.51
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Formule C23H15F2N3O6S2
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SMILES
O=C(NC1=CC=C(S(NC(NC2=CC=C3OC(F)(OC3=C2)F)=O)(=O)=O)C=C1)C4=CSC5=C4C=CC=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)