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

For research use only. We do not sell to patients.

PDE4-IN-34

PDE4-IN-34 Chemical Structure

CAS No. : 3052591-16-6

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PDE4-IN-34 Related Antibodies

Top Publications Citing Use of Products

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

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[1].

IC50 & Target[1]

PDE4B1

19 pM (IC50)

PDE4D2

14 pM (IC50)

PDE8A1

4.092 μM (IC50)

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-t AUC0-∞ MRT0-t MRT0-∞ Bioavailability Vz CL
Rat[1] 3 mg/kg i.v. 754 ng/mL 0.083 h 4.46 h 4458 ng·h/mL 4919 ng·h/mL 4.80 h 6.39 h / 4317 mL/kg 681 mL/h/kg
Rat[1] 10 mg/kg p.o. 92.0 ng/mL 1.5 h 10.3 h 1225 ng·h/mL 1637 ng·h/mL 8.45 h 14.7 h 9.99 % / /
In Vivo

PDE4-IN-34 (Compound P29) (0.1-3 μmol/kg; intratracheal inhalation; once daily; 28 days) dose-dependently alleviates cigarette smoke- and LPS-induced COPD in rats by suppressing inflammatory cell activity and cytokine release, with maximal effects observed at the 3 μmol/kg intratracheal dose administered daily for 28 days[1].
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.

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]
Dosage: 0.1 μmol/kg; 1 μmol/kg; 3 μmol/kg
Administration: intratracheal inhalation; once daily; 28 days
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.
Molecular Weight

381.64

Formula

C17H11Cl3N2O2
CAS No.
SMILES

ClC1=NC2=C(C(C(CC3=C(C=NC=C3Cl)Cl)=O)=CC=C2OC)C=C1
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-34 Related Classifications

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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-343052591-16-6Phosphodiesterase (PDE)TNF ReceptorTumor Necrosis Factor ReceptorTNFRPDE4D2 enzymephosphodiesterase 4rat modelschronic obstructive pulmonary diseaseperipheral blood mononuclear cellshuman PBMCsPDE4B1 enzymePDE4human PDE4human liver microsomesInhibitorinhibitorinhibit

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