1. Metabolic Enzyme/Protease
  2. FBPase
  3. 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.

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

FBPase-IN-7

FBPase-IN-7 Chemical Structure

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Description

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[1].

In Vitro

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.

In Vivo

FBPase-IN-7 (Compound 29) (100 mg/kg; i.p.; single dose) produces meaningful glycemic control in vivo, reducing the 0-1.5 h blood glucose area under the curve by 20.6% in fasted ICR mice subjected to an oral glucose tolerance test[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice with glucose challenge (2 g/kg) (male, 20-24 g, 12 h-fasted, oral glucose tolerance test model)[1]
Dosage: 100 mg/kg
Administration: i.p.; single dose
Result: Reduced the blood glucose AUC0-1.5ₕ by 20.6%.
Molecular Weight

531.51

Formula

C23H15F2N3O6S2

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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Room temperature in continental US; may vary elsewhere.

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

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
FBPase-IN-7
Cat. No.:
HY-182346
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