D 22888
D 22888 is an orally active PDE4 inhibitor, with human PDE4 IC50 of 0.153 μM, and selectivity over PDE3 and PDE5. D 22888 elevates intracellular cAMP levels to modulate target cell functions. D 22888 acts as a relaxant of human bronchial ring inherent tone. D 22888 inhibits opsonized zymosan-induced superoxide anion generation by human eosinophils. D 22888 reduces bronchoalveolar lavage eosinophil numbers in allergen-challenged sensitized guinea pigs via single or chronic oral dosing. D 22888 can be used for the research of bronchial asthma.
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: 182282-60-6
- 分子式: C16H20N4O2
- 分子量:300.36
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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
製品説明
IC50 & Target
[1]|
PDE4 0.153 μM (IC50) |
体外実験
D-22888 potently and selectively inhibits human PMNL PDE4 with an IC50 of 153 nM, exhibiting much weaker inhibition of human platelet PDE3 and PDE5[1].
D-22888 (up to 10 μM; equilibration for each concentration until response stabilized) has minimal effect on PGF2α-induced tone in human pulmonary artery rings at concentrations up to 10 μM[1].
D-22888 (1-10 μM; 5 min pre-incubation, followed by 30 min incubation with opsonized zymosan (OZ)) inhibits opsonized zymosan-induced superoxide anion generation in human eosinophils in a concentration-dependent manner with an IC50 of 3.1 μM[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:Dunkin-Hartley (male, 200-250 g, actively sensitized with two subcutaneous injections of 10 μg ovalbumin + 1 mg Al(OH)3 14 days apart, challenged with ovalbumin aerosol 7 days after the second injection)[1]
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Dosage:10 mg/kg (pre-challenge single dose); 30 mg/kg (pre-challenge single dose); 30 mg/kg (post-challenge single dose); 30 mg/kg (twice daily for 3 days)
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Administration:p.o. (single dose 2 h pre-challenge); p.o. (single dose 4 h post-challenge); p.o. (twice daily for 3 days, last dose 2 h pre-challenge)
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Result:Reduced allergen-induced bronchoalveolar lavage eosinophilia by 48%.
Reduced allergen-induced bronchoalveolar lavage eosinophilia by 73%.
Reduced allergen-induced bronchoalveolar lavage eosinophilia by 68%.
Reduced allergen-induced bronchoalveolar lavage eosinophilia by 88%.
化学情報
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CAS 番号 182282-60-6
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分子量 300.36
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分子式 C16H20N4O2
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SMILES
O=C1C2=C(C)N=C(CC)N2C3=NC(OC)=CC=C3N1CCC
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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)
D 22888 関連分類
HY-183463 関連分類
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