PDE4-IN-30
PDE4-IN-30 is a selective PDE4 inhibitor with an IC50 of 2.7 nM for PED4D2, targeting PDE4 through halogen bonding and metal coordination. PDE4-IN-30 exhibits at least 67-fold selectivity for other PDE subfamilies. PDE4-IN-30 can be used for the research of idiopathic pulmonary fibrosis.
For research use only. We do not sell to patients.
- Formula: C14H17BrN8O2
- Molecular Weight:409.24
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PDE4D2 2.7 nM (IC50) |
PDE10A 181.8 nM (IC50) |
PDE8A 1156 nM (IC50) |
PDE5A 7491 nM (IC50) |
PDE4-IN-30 (compound 13c) (5-20 μM; 48 hours) effectively inhibits TGF-β1-induced fibroblast-to-myofibroblast transition (FMT) and epithelial-mesenchymal\r
transition (EMT) in MRC-5 and A549 cells[1].
PDE4-IN-30 (5-20 μM; 48 hours) significantly attenuates TGF-β1-induced A549 cell proliferation and cell migration[1].
PDE4-IN-30 exhibits good cell permeability and favorable drug-likeness properties in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MRC-5 and A549 cell lines
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:48 h
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Result:Significantly inhibited the overexpression of α-smooth muscle actin (α-SMA), COL1A1, and FN markers.
Downregulatedthe expression of N-cadherin and vimentin while it restored E-cadherin. expression to baseline levels.
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Cell Line:A549 cell lines
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:48 h
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Result:Significantly attenuated TGF-β1-induced A549 cell proliferation and migration.
| Species | Dose | Route | Note | Cmax | Tmax | T1/2 | AUC0-t | CL |
|---|---|---|---|---|---|---|---|---|
| Mice | 2.5 mg/kg | i.v. | 文献审核 | 104 ng/mL | 0.0833 h | 0.0737 h | 25.8 ng·h/mL | 110268 mL/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J (6-8 weeks old; 18-22 g) were induced by a single intratracheal instillation of BLM (3 mg/kg)[1]
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Dosage:2.5 mg/kg
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Administration:Intraperitoneal injection; 3 weeks of treatment starting from the second day post-BLM induction
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Result:Significantly reduced lung coefficient, hydroxyproline levels, and fibrotic markers (FN1, COL1A1, α-SMA, N-cadherin, vimentin) while increasing E-cadherin expression.
Improved lung function parameters (inspiratory capacity (IC), forced vital capacity (FVC), lung compliance (Cchord), vital capacity (VC), peakexpiratory flow (PEF)) and reduced airway resistance.
Histological analysis showed reduced alveolar fibrosis and inflammatory infiltration.
Chemical Information
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Molecular Weight 409.24
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Formula C14H17BrN8O2
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SMILES
NC1=C(C(NCCCC(NO)=O)=NC2=C(C=NN12)C3=CN(N=C3)C)Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE4-IN-30 Related Classifications
HY-179639 Related Classifications
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