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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- 화학식: C23H15F2N3O6S2
- 분자량:531.51
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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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분자량 531.51
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)