HIF-1α-IN-8
HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC50 of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE).
For research use only. We do not sell to patients.
- Formula: C29H30FNO7
- Molecular Weight:523.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HIF-1α 2.02 μM (IC50) |
IKKα |
HIF-1α-IN-8 (Compound N41) (20 μM, 48 h) suppresses the secretion of inflammatory factors IL-6 and NO in C8-D1A cells[1].
HIF-1α-IN-8 (5-50 μM, 12 h) reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells[1].
HIF-1α-IN-8 (5-20 μM, 24 h) inhibits the expression of key proteins (HIF-1α, IKKα, p65, IκBα) in the HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins MMP-9 and AQP-4 in C8-D1A cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C8-D1A cells
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Concentration:5, 10, 20, 50 μM
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Incubation Time:12 h
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Result:Reduced apoptosis in C8-D1A cells.
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Cell Line:C8-D1A cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 h
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Result:Inhibited the expression of key proteins (HIF-1α, IKKα, p65, IκBα) in the HIF-1α/IKKα/NF-κB signaling pathway.
Reduced the expression of blood-brain barrier permeability-related proteins MMP-9 and AQP-4 in C8-D1A cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male C57BL/6 mice were intraperitoneally injected with 0.5 mg/kg LPS (HY-D1056) and after 30 min of adaptation, mice were placed in a ProOx-810 Animal Low-Pressure Oxygen Control System to simulate a 7000 m high-altitude environment for 12 h to establish the HACE model[1]
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Dosage:25 mg/kg, 50 mg/kg, 100 mg/kg
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Administration:i.g. once daily, 3 days
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Result:Reduced weight loss in a dose-dependent manner.
Decreased brain water content (BWC) dose-dependently.
Regulated oxidative stress in brain tissue.
Suppressed inflammatory factor (IL-6, TNF-α)levels.
Alleviated brain tissue pathological damage.
Inhibited protein expression in the HIF-1α/IKKα/NF-κB signaling pathway.
Chemical Information
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Molecular Weight 523.55
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Formula C29H30FNO7
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SMILES
O=C(NC1=CC=C(C2=CC=C(CCO[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O3)C=C2)C=C1)/C=C/C4=CC=CC=C4F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)