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.
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- CAS No.: 182282-60-6
- Formule: C16H20N4O2
- Masse moléculaire:300.36
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
PDE4 0.153 μM (IC50) |
In Vitro
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.
In Vivo
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%.
Chemical Information
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CAS No. 182282-60-6
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Masse moléculaire 300.36
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Formule C16H20N4O2
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SMILES
O=C1C2=C(C)N=C(CC)N2C3=NC(OC)=CC=C3N1CCC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
D 22888 Related Classifications
HY-183463 Related Classifications
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