NuP-3
NuP-3 is an orally active dual inhibitor of MAPK13 (IC50 < 250 nM), MAPK14 (IC50 = 7 nM), MAPK12 and MAPK11. NuP-3 blocks airway inflammation and mucus production. NuP-3 is used for the research of respiratory system diseases.
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: 2392969-05-8
- 分子式: C24H24ClFN4O3
- 分子量:470.92
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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
- プロトコル
- 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
製品説明
体外実験
NuP-3 (21 days) inhibits MUC5AC production in primary porcine tracheobronchial epithelial cells stimulated by IL-13, with an IC50 of 0.420 nM within 21 days and a cellular therapeutic index of 2381, indicating low toxicity[1].
NuP-3 (21 days) potently inhibits MUC5AC production in primary human tracheobronchial epithelial cells stimulated by IL-13, with an IC50 of 0.005 nM within 21 days and a cell therapeutic index of 200000, indicating high safety[1].
NuP-3 (Compound 396) at 0.1 μM selectively inhibits MAPK13, MAPK14, MAPK11, and MAPK12; in a cell-free kinome screening, only 4% of the 400 tested kinases show an inhibition rate > 90%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Yucatan mini-pigs (male and female, 7-8 weeks of age, 21-25 kg, IL-13-challenged model)[1]
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Dosage:0.2 mg/kg; 2 mg/kg; 20 mg/kg
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Administration:p.o.; twice daily; 6 days
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Result:Significantly decreased BAL fluid levels of MUC5AC and CLCA1, and significantly reduced eosinophil and neutrophil influx into the airspace at 2 mg/kg compared to vehicle control.
Showed decreased anti-mucus and anti-inflammatory effects at 0.2 mg/kg and preserved effects at 20 mg/kg compared to vehicle control.
Observed no adverse effects (behavior, appetite, body weight, vital signs, gastrointestinal/urinary function, complete blood count) at any dose.
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Animal Model:Yucatan mini-pigs (male and female, 7-8 weeks of age, 21-25 kg, Sendai virus-infected model)[1]
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Dosage:2 mg/kg
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Administration:p.o.; twice daily; 24 days
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Result:Significantly attenuated SeV-induced increases in BAL fluid levels of MUC5AC and CLCA1 compared to vehicle control.
Did not alter viral titer or cause detectable adverse effects.
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Animal Model:Mice[1]
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Dosage:2 mg/kg
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Administration:i.p.; twice daily; 23 days (pre-infection); twice daily; 11 days (delayed post-infection)
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Result:Fully blocked SeV-induced increases in lung tissue Muc5ac, Clca1, Aqp3, Krt5, Trp63, Il33, Il13, and Arg1 mRNA levels compared to vehicle control when administered starting 2 days before infection.
Significantly attenuated the aforementioned mRNA levels compared to vehicle control when treatment was delayed until 10 days post-infection.
Did not affect mouse behavior, body weight, or clinical signs of infection.
化学情報
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CAS 番号 2392969-05-8
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分子量 470.92
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分子式 C24H24ClFN4O3
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SMILES
O=C(NC1=CC(C(C)(C)C)=CC=C1Cl)NC2=CC=C(C=C2F)OC3=CC(NC(C)=O)=NC=C3
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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)
NuP-3 関連分類
HY-186241 関連分類
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