2. Metabolic Enzyme/Protease GPCR/G Protein Epigenetics Cell Cycle/DNA Damage Apoptosis Immunology/Inflammation
  3. Phosphodiesterase (PDE) Adenosine Receptor HDAC Apoptosis Interleukin Related TNF Receptor Endogenous Metabolite
  4. Theophylline

Theophylline  (Synonyms: 1,3-Dimethylxanthine; Theo-24)

Cat. No.: HY-B0809 Purity: 99.89%
COA Handling Instructions

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Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.

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

Theophylline Chemical Structure

Theophylline Chemical Structure

CAS No. : 58-55-9

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10 mM * 1 mL in DMSO
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Based on 6 publication(s) in Google Scholar

Other Forms of Theophylline:

Theophylline 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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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].

IC50 & Target

IL-10

 

IL-6

 

PDE3

 

Human Endogenous Metabolite

 

In Vitro

Theophylline (1,3-Dimethylxanthine) (1-1000 µM) inhibits cAMP hydrolysis by PDE in homogenates of bronchial tissue to relax human bronchus and pulmonary arteries[1].
Theophylline (1,3-Dimethylxanthine) (10 µg/mL; 24 h; eosinophils) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2[2].
Theophylline (1,3-Dimethylxanthine) (0-500 µM; 2 h; A549 cells) inhibits NF-κB activation, I kappa B alpha (I-κBα) degradation and decreases the level of IL-6 in a concentration-dependent manner[3].
Theophylline (1,3-Dimethylxanthine) (0-1000 µM; 30 min; A549 cells) induces histone deacetylase activity to decrease inflammatory gene expression[4].

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

Theophylline Related Antibodies

Western Blot Analysis[3]

Cell Line: A549 cells
Concentration: 0, 20, 100 and 500 µM
Incubation Time: 2 hours
Result: Decreased the expression of NF-κB p65 and I-κBα degradation in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: Eosinophils
Concentration: 10 µg/mL
Incubation Time: 24 hours
Result: Decreased the expression of Bcl-2.
In Vivo

Theophylline (1,3-Dimethylxanthine) (100 mg/kg; i.p.; daily, for 9 d; male Swiss mice) has anti-inflammatory activity in mice and increases IL-6 and IL-10 levels and inhibits TNF-α and NO[1].

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

Animal Model: Male Swiss mice[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection; daily, for 9 days
Result: Increased IL-6 and IL-10 levels and inhibited TNF-α and NO.
Clinical Trial
Molecular Weight

180.16

Formula

C7H8N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C)N(C)C2=C(N=CN2)C1=O
Structure Classification
Initial Source
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: 

0.1 M NaOH : 20 mg/mL (111.01 mM; ultrasonic and warming and adjust pH to 10 with 0.1 M NaOH and heat to 60°C)

DMSO : 11.11 mg/mL (61.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 5 mg/mL (27.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.5506 mL 27.7531 mL 55.5062 mL
5 mM 1.1101 mL 5.5506 mL 11.1012 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 1.11 mg/mL (6.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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: ≥ 1.11 mg/mL (6.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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: 11 mg/mL (61.06 mM); Clear solution; Need ultrasonic

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

COA (253 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
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 / 0.1 M NaOH 1 mM 5.5506 mL 27.7531 mL 55.5062 mL 138.7655 mL
5 mM 1.1101 mL 5.5506 mL 11.1012 mL 27.7531 mL
10 mM 0.5551 mL 2.7753 mL 5.5506 mL 13.8766 mL
15 mM 0.3700 mL 1.8502 mL 3.7004 mL 9.2510 mL
20 mM 0.2775 mL 1.3877 mL 2.7753 mL 6.9383 mL
25 mM 0.2220 mL 1.1101 mL 2.2202 mL 5.5506 mL
DMSO / 0.1 M NaOH 30 mM 0.1850 mL 0.9251 mL 1.8502 mL 4.6255 mL
40 mM 0.1388 mL 0.6938 mL 1.3877 mL 3.4691 mL
50 mM 0.1110 mL 0.5551 mL 1.1101 mL 2.7753 mL
60 mM 0.0925 mL 0.4626 mL 0.9251 mL 2.3128 mL
0.1 M NaOH 80 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7346 mL
100 mM 0.0555 mL 0.2775 mL 0.5551 mL 1.3877 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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Theophylline 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:

Theophylline58-55-91,3-Dimethylxanthine Theo-24Theo24Theo 24Theo-24Phosphodiesterase (PDE)Adenosine ReceptorHDACApoptosisInterleukin RelatedTNF ReceptorEndogenous MetaboliteP1 receptorHistone deacetylasesILTumor Necrosis Factor ReceptorTNFRairway smooth muscleNF-κBI-κBαasthmachronic obstructive pulmonary diseaseA549 cellseosinophilsInhibitorinhibitorinhibit

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