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.
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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。
- CAS 番号: 2499855-36-4
- 分子式: C22H26N4O4
- 分子量:410.47
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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.
化学情報
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CAS 番号 2499855-36-4
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分子量 410.47
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分子式 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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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)
GLPG4471 関連分類
HY-178012 関連分類
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