Anti-inflammatory agent 79
Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body.
For research use only. We do not sell to patients.
- Formula: C21H17NO2
- Molecular Weight:315.37
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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 .55 μM (IC50, [1]) |
Anti-inflammatory agent 79 (2.5-10 μM; 24 h) can concentration-dependently block hypoxia-induced HIF-1α protein accumulation, reduce inflammatory response, inhibit cell invasiveness and promote VHL-dependent HIF-1α degradation in human RA synovial cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MH7A cells
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Decreased the protein level of HIF-1α
Decreased the secretion of cytokines, including IL-1β, IL-6 and TNF-α.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adjuvant-induced arthritic (AIA) model in SD rats[1]
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Dosage:30 mg/kg, 60 mg/kg
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Administration:ip; once per two days; from 13 to 29 days after CFA injection (vehicle: 5 % ethanol and 5 % cremophor EL in FBS)
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Result:Attenuated the development and severity of arthritis
Significantly decreased the HIF-1α expression and the percentage of HIF-1α positive cells.
Chemical Information
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Molecular Weight 315.37
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Formula C21H17NO2
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SMILES
O=C(C1=CC=C(C2=COC=C2)C=C1C=C3)N3CCC4=CC=CC=C4
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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)