PDE4-IN-34
PDE4-IN-34 is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 19 pM and 14 pM against PDE4B1 and PDE4D2, respectively. PDE4-IN-34 shows weak inhibitory activity against PDE8A1, with an IC50 value of 4.092 μM, and exhibits significant selectivity over other subtypes (IC50 > 10 μM). PDE4-IN-34 improves pulmonary function, reduces inflammatory responses and alleviates lung tissue damage in a rat model induced by cigarette smoke combined with LPS (HY-D1056). PDE4-IN-34 can be used for research related to chronic obstructive pulmonary disease.
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- CAS No.: 3052591-16-6
- 화학식: C17H11Cl3N2O2
- 분자량:381.64
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보관:
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PDE4B1 19 pM (IC50) |
PDE4D2 14 pM (IC50) |
PDE8A1 4.092 μM (IC50) |
PDE4-IN-34 (Compound P29) (1 fM-1 µM; 18 h) potently inhibits LPS-induced TNF-α release in human peripheral blood mononuclear cells (PBMCs), with an IC50 of 0.3 nM[1].
PDE4-IN-34 (1 μM; 6 h) binds to 99.5% of human plasma proteins at a concentration of 1 μM[1].
PDE4-IN-34 (1 μM) is metabolized in human liver microsomes, with a hepatic clearance rate of 0.0522 mL/min/mg and a half-life of 26.6 min[1].
PDE4-IN-34 does not significantly inhibit hERG potassium channels at concentrations up to 30 μM, indicating a low risk of cardiotoxicity[1].
PDE4-IN-34 does not significantly inhibit human liver CYP1A2, CYP2C9, CYP2C19, CYP2D6 or CYP3A4 enzymes at concentrations up to 10 μM, suggesting a low risk of drug-drug interactions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PDE4-IN-34 (3-10 mg/kg; inhaled; single daily dose) does not induce emesis in beagle dogs at inhaled doses up to 10 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male, 200-250 g, COPD induced by intratracheal LPS instillation on days 1 and 14 plus daily cigarette smoke exposure from days 2 to 28)[1]
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Dosage:0.1 μmol/kg; 1 μmol/kg; 3 μmol/kg
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Administration:intratracheal inhalation; once daily; 28 days
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Result:Produced a dose-dependent reduction in white blood cell counts, eosinophils, neutrophils, and lymphocytes in BALF.
Caused a dose-dependent reduction in inflammatory markers including IL-1β, TNF-α, and IL-6 in serum, lung tissue, and BALF, with significant effects observed at 1 μmol/kg and maximal effects at 3 μmol/kg.
Led to notable improvements in lung structure at 3 μmol/kg dose, with reduced alveolar wall disruption, interstitial thickening, and inflammatory cell infiltration compared to the vehicle-treated group.
Showed significantly reduced inflammatory cell infiltration at 0.1 and 1 μmol/kg doses relative to the vehicle group.
Chemical Information
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CAS No. 3052591-16-6
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분자량 381.64
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화학식 C17H11Cl3N2O2
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SMILES
ClC1=NC2=C(C(C(CC3=C(C=NC=C3Cl)Cl)=O)=CC=C2OC)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE4-IN-34 Related Classifications
HY-181646 Related Classifications
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