IRAK4-IN-18
IRAK4-IN-18 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 15 nM. IRAK4-IN-18 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-18 can be used for researching arthritis disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 3032075-26-3
- 分子式: C24H25FN6O3
- 分子量:464.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
IRAK4 15 nM (IC50) |
体外実験
IRAK4-IN-18 (compound 33) has inhibitory activity against LPS-induced IL23 in THP and DC with IC50s of 0.25 and 0.14 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
IRAK4-IN-18 (1 mg/kg for IV, 5 mg/kg for PO, single dosage) exhibits a favorable pharmacokinetics profile with a clearance of 53 mL/min/kg and oral bioavailability of 38%[1].
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) rat models[1]
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Dosage:5, 10 and 20 mg/kg
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Administration:twice daily for 21 days
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Result:Completely stopped arthritis development based on hind paw clinical scores at 30 mg/kg dose, twice daily, and effectively decreased disease progression with 97% inhibition at 20 mg/kg dose, 56% inhibition at 10 mg/kg dose and 30% inhibition at 5 mg/kg dose.
化学情報
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CAS 番号 3032075-26-3
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分子量 464.49
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分子式 C24H25FN6O3
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SMILES
O=C(N)[C@@H]1[C@@H]([C@@H]2C[C@H]1C=C2)NC3=NC(NC4=CC(N5CCOCC5)=CC(F)=C4)=NC6=C3OC=C6
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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)