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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C23H15F2N3O6S2
- 分子量:531.51
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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%.
化学情報
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分子量 531.51
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)