2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. 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.

PDE4-IN-30

PDE4-IN-30 Chemical Structure

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PDE4-IN-30 Related Antibodies

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Description

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[1].

IC50 & Target[1]

PDE4D2

2.7 nM (IC50)

PDE10A

181.8 nM (IC50)

PDE8A

1156 nM (IC50)

PDE5A

7491 nM (IC50)

In Vitro

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.

PDE4-IN-30 Related Antibodies

Western Blot Analysis[1]

Cell Line: MRC-5 and A549 cell lines
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 48 h
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.

Cell Proliferation Assay[1]

Cell Line: A549 cell lines
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 48 h
Result: Significantly attenuated TGF-β1-induced A549 cell proliferation and migration.
Parmacokinetics
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
In Vivo

PDE4-IN-30 (compound 13c) (2.5 mg/kg, intraperitoneal injection; 3 weeks of treatment) ameliorates Bleomycin (BLM) (HY-17565A)-induced pulmonary fibrosis in C57BL/6J (6-8 weeks old) mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 2.5 mg/kg
Administration: Intraperitoneal injection; 3 weeks of treatment starting from the second day post-BLM induction
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. 
Molecular Weight

409.24

Formula

C14H17BrN8O2
SMILES

NC1=C(C(NCCCC(NO)=O)=NC2=C(C=NN12)C3=CN(N=C3)C)Br
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PDE4-IN-30 Related Classifications

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× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PDE4-IN-30Phosphodiesterase (PDE)PDE4 inhibitorantifibrotic activitypotency enhancementhigh affinitypyrazolo[1,5-]pyrimidinehalogen-bindinghepatic microsomal stabilitypulmonary fibrosisPDE4metal-coordinationInhibitorinhibitorinhibit

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