HPA-IN-3
HPA-IN-3 (compound 5) is a heparanase (HPA) inhibitor with an IC50 of 11.27 μM against human targets. HPA-IN-3 binds to the active site of HPA, and its structural features enhance binding stability and affinity. HPA-IN-3 reduces the levels of proinflammatory cytokines. HPA-IN-3 maintains organ morphology. HPA-IN-3 improves the survival rate of mice with sepsis induced by cecal ligation and puncture. HPA-IN-3 can be used in studies related to sepsis.
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- Formule: C25H32N2Na10O45S8
- Masse moléculaire:1566.93
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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hHPA 11.27 μM (IC50) |
HPA-IN-3 (compound 5) (0-1000 μM; 10 min pre-incubation with HPA, 30 min incubation with substrate) potently inhibits recombinant active heparanase with an IC50 of 11.27 μM[1].
HPA-IN-3 (0-10000 μM; 3 min) shows minimal interference with the intrinsic coagulation cascade, with no significant aPTT prolongation observed at concentrations up to 10000 μM[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:C57BL/6J (male, 6-8 weeks old, 20-25 g, CLP-induced sepsis model)[1]
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Dosage:40 mg/kg
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Administration:s.c.; single dose
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Result:Achieved a 60% survival rate over 120 hours.
Reduced serum levels of TNF-α, IL-6, and IL-1β.
Decreased inflammatory infiltrates and preserved tissue architecture in lung and kidney tissues.
Lowered lung and kidney injury scores significantly relative to the CLP control group.
Chemical Information
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Masse moléculaire 1566.93
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Formule C25H32N2Na10O45S8
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SMILES
O[C@@H]1[C@@H](OS(=O)(O[Na])=O)[C@H](OS(=O)(O[Na])=O)[C@@H](C(O[Na])=O)O[C@H]1O[C@H]2[C@H](COS(=O)(O[Na])=O)OC(OC3[C@H](C(O[Na])=O)OC(O[C@H]4C(O)[C@@H](NS(=O)(O[Na])=O)[C@@H](OC)O[C@@H]4COS(=O)(O[Na])=O)[C@H](OS(=O)(O[Na])=O)[C@H]3O)[C@@H](NS(=O)(O[Na])=O)[C@@H]2OS(=O)(O[Na])=O
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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)
HPA-IN-3 Related Classifications
HY-184684 Related Classifications
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