2. GPCR/G Protein Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Adenosine Receptor Phosphodiesterase (PDE) Reactive Oxygen Species
  4. Doxofylline

Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm.

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Doxofylline Chemical Structure

Doxofylline Chemical Structure

CAS No. : 69975-86-6

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Based on 1 publication(s) in Google Scholar

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Doxofylline Related Antibodies

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Description

Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm[1][2][3].

IC50 & Target

Adenosine A1 receptor, phosphodiesterase IV[1][2][3].
In Vitro

Doxofylline (5, 10 µM; 48 h) shows potent protection against LPS-induced epithelial inflammation by reducing PGE2, NO release, and decreasing mitochondrial ROS generation in 16HBE cells[1].
Doxofylline (5, 10 µM; 48 h) suppresses LPS-induced expression of NADPH oxidase subunits and TXNIP 16HBE cells[1].
Doxofylline (5, 10 µM; 48 h) inhibits LPS-induced NLRP3 inflammasome activation and secretion of IL-1b and IL-18, as well as mitigates LPS-mediated SIRT1 reduction[1].
Doxofylline (0.1-10 µM; 15 min) significantly reduces fMLP-induced leukocyte migration in BM cells (fMLP: Formyl-Methionyl-Leucyl-Phenylalanine)[2].

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

Doxofylline Related Antibodies

Cell Viability Assay[1]

Cell Line: 16HBE cells
Concentration: 5, 10 µM
Incubation Time: 48 h
Result: Weakened LPS-induced NO and PGE2 in a dose-dependent manner.
Exerted dose-dependent inhibition on LPS-induced mitochondrial ROS production and NADPH oxidase subunits expression.
Suppressed LPS-induced TXNIP expression and NLRP3 inflammasome activation at the protein level in a dose-dependent manner.
Inhibited LPS-induced secretion of IL-1b and IL-18.

Cell Viability Assay[2]

Cell Line: BM cells (from naive mice)
Concentration: 0.1-10 µM
Incubation Time: 15 min (pretreat)
Result: Notably surpressed positive migration of BM cells in response to fMLP.
In Vivo

Doxofylline (0.3, 1 mg/kg; i.p.; single) inhibits LPS-induced inflammation in the lungs of mice[2].
Doxofylline (0.3 mg/kg; i.p.; pre-treat; single) notably reduces the adhesion of cells to the vascular tissue and surpresses the expression of LPS-induced ICAM-1 in vivo[2].

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

Animal Model: Male BALB/c mice (6 to 8-week-old)[2].
Dosage: 0.3, 1 mg/kg
Administration: Intraperitoneal injection; single.
Result: Significantly inhibited the migration of neutrophils and the release of IL-6 and TNF-a into the lung lumen.
Increased the bone marrow leukocyte numbers to levels similar to those seen in the saline-treated group.
Notably reduced the number of circulating leukocytes in comparison to LPS-treated mice.
Significantly reduced accumulation of neutrophils in the peribronchial area.
Animal Model: Male BALB/c mice (6 to 8-week-old)[2].
Dosage: 0.3 mg/kg
Administration: Intraperitoneal injection; pre-treat; single.
Result: Significantly reduced the adhesion of cells to the vascular tissue, but not the rolling of cells along the vessel wall in mice.
Significantly reduced the expression of ICAM-1 induced by LPS.
Clinical Trial
Molecular Weight

266.25

Formula

C11H14N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C)N(C)C2=C(N(CC3OCCO3)C=N2)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (187.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (93.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7559 mL 18.7793 mL 37.5587 mL
5 mM 0.7512 mL 3.7559 mL 7.5117 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 65 mg/mL (244.13 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.7559 mL 18.7793 mL 37.5587 mL 93.8967 mL
5 mM 0.7512 mL 3.7559 mL 7.5117 mL 18.7793 mL
10 mM 0.3756 mL 1.8779 mL 3.7559 mL 9.3897 mL
15 mM 0.2504 mL 1.2520 mL 2.5039 mL 6.2598 mL
20 mM 0.1878 mL 0.9390 mL 1.8779 mL 4.6948 mL
25 mM 0.1502 mL 0.7512 mL 1.5023 mL 3.7559 mL
30 mM 0.1252 mL 0.6260 mL 1.2520 mL 3.1299 mL
40 mM 0.0939 mL 0.4695 mL 0.9390 mL 2.3474 mL
50 mM 0.0751 mL 0.3756 mL 0.7512 mL 1.8779 mL
60 mM 0.0626 mL 0.3130 mL 0.6260 mL 1.5649 mL
80 mM 0.0469 mL 0.2347 mL 0.4695 mL 1.1737 mL
DMSO 100 mM 0.0376 mL 0.1878 mL 0.3756 mL 0.9390 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Doxofylline Related Classifications

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:

Doxofylline69975-86-6Adenosine ReceptorPhosphodiesterase (PDE)Reactive Oxygen SpeciesP1 receptorasthmabronchitisCOPD16HBE cellsBM cellsbronchospasmInhibitorinhibitorinhibit

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