GLPG4471
GLPG4471 is a selective and orally active IRAK4 inhibitor with an IC50 of 1.7 nM. GLPG4471 exhibits potent inhibition of cytokine (TNFα and IFNα) secretion in cellular and whole blood phenotypic assays. GLPG4471 displays significant activity in a mouse model of collagen-induced arthritis. GLPG4471 can be used for the study of arthritis.
For research use only. We do not sell to patients.
- CAS No.: 2499855-36-4
- Formula: C22H26N4O4
- Molecular Weight:410.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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IRAK4 1.7 nM (IC50) |
GLPG4471 potently inhibits secretion of TNFα and IFNα in human whole blood and PBMCs stimulated with CL097 (HY-128799)[1].
GLPG4471 exhibits excellent metabolic stability in the liver microsomes and liver cells of mice, rats and humans, and the predicted hepatic clearance rate was low to moderate[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:Collagen-induced arthritis (CIA) model established in mice[1]
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Dosage:3, 10, 30 mg/kg
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Administration:Oral administration (p.o.), twice daily for 17 days
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Result:Exhibited a dose-dependent manner of significantly inhibiting the progression of arthritis.
Was above mouse whole blood IC50 for 15, 19 and 24 h at 3, 10 and 30 mg/kg twice-daily, respectively.
Chemical Information
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CAS No. 2499855-36-4
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Molecular Weight 410.47
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Formula C22H26N4O4
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SMILES
COC1=CN2N=C(C=C2C=C1NC(C3=CC=CN(C3=O)C4CC4)=O)CCC(C)(O)C
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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)