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

Etofylline  (Synonyms: 7-(β-Hydroxyethyl)theophylline)

Cat. No.: HY-B1209 Purity: 99.72%
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Etofylline (7-(β-Hydroxyethyl) theophylline) is an oral bronchodilator with anti-inflammatory effects. Etofylline inhibits phosphodiesterase and prevents the degradation of cAMP (cyclic adenosine monophosphate), leading to smooth muscle relaxation, reducing inflammatory responses and improving respiratory function. Etofylline affects the development of zebrafish embryos.

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Etofylline Chemical Structure

Etofylline Chemical Structure

CAS No. : 519-37-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 55 In-stock
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Solid
500 mg USD 50 In-stock
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Other Forms of Etofylline:

Etofylline Related Antibodies

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Description

Etofylline (7-(β-Hydroxyethyl) theophylline) is an oral bronchodilator with anti-inflammatory effects. Etofylline inhibits phosphodiesterase and prevents the degradation of cAMP (cyclic adenosine monophosphate), leading to smooth muscle relaxation, reducing inflammatory responses and improving respiratory function. Etofylline affects the development of zebrafish embryos[1][2][3].

In Vivo

Etofylline (1 mg/kg, intratracheal administration) can be delivered into rat lungs after being coated with Mannose-anchored N,N,N-trimethyl chitosan nanoparticles and is safe for pulmonary administration[2].
Etofylline (100-1000 mg/L, incubate in diluent; 24, 48 and 72 h post fertilization) affects the locomotor activity and development of zebrafish embryos[3].
Pharmacokinetic parameters of ethoxyphylline (150 mg/kg within 5 minutes) in rabbits after intravenous injection [1]

Compartment β(h-1) α(h-1) γ(h-1) Vdβ Cl(1/kg/h) t1/2 (h) 1/MRTb(h-14) Vdss (1/kg) MRTb(h-14)
two 0.41±0.09 4.72±1.57 / 1.41±0.31 0.37±0.12 1.7 / / /
three 0.39±0.13 1.68±0.87 19.99±6.78 1.03±0.34 0.39±0.08 1.8 / / /
none / / / / 0.37±0.08 / 0.59±0.24 0.71±0.30 1.94±0.7

Pulmonary pharmacokinetic parameters after intratracheal administration of suspension and Etofylline-loaded NPs formulations[1]
Group Cmax (ng/mL) Tmax (min) AUC(0-480) (min·ng/mL) AUC(0-∞) (min·ng/mL) MRT (min)
Etofylline suspension 1845 15 14582101 21528427 2.04
Etofylline-TMC-TPP NPs 86437 60 68723641 91852140 52.15
Etofylline-MnTMC-TPP NPs 78162 60 64521708 89426410 62.27

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

Animal Model: Zebrafish embryos[3]
Dosage: 600 mg/L; 100, 200, 400, 600, 1000 mg/L
Administration: Incubate in diluent; 24, 48 and 72 h post fertilization
Result: Caused curling and contraction of embryos at 24 hours, impaired vitality of embryos at 48 and 72 hours, and slowed swimming speed. It affects somite formation, produces movement defects, abnormal heartbeat, abnormal blood circulation and deformities.
Showed TC50 of 1058mg/L, TC50 of GMS (General Morphological defect Score) of 848mg/L and TC50 of GTS (General Teratogenic effect Score) of 892mg/L.
Molecular Weight

224.22

Formula

C9H12N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C)N(C)C2=C(N(CCO)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: 

H2O : 50 mg/mL (223.00 mM; Need ultrasonic)

DMSO : 25 mg/mL (111.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4599 mL 22.2995 mL 44.5991 mL
5 mM 0.8920 mL 4.4599 mL 8.9198 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.

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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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: ≥ 2.5 mg/mL (11.15 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 (11.15 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: 50 mg/mL (223.00 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.
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
DMSO / H2O 1 mM 4.4599 mL 22.2995 mL 44.5991 mL 111.4976 mL
5 mM 0.8920 mL 4.4599 mL 8.9198 mL 22.2995 mL
10 mM 0.4460 mL 2.2300 mL 4.4599 mL 11.1498 mL
15 mM 0.2973 mL 1.4866 mL 2.9733 mL 7.4332 mL
20 mM 0.2230 mL 1.1150 mL 2.2300 mL 5.5749 mL
25 mM 0.1784 mL 0.8920 mL 1.7840 mL 4.4599 mL
30 mM 0.1487 mL 0.7433 mL 1.4866 mL 3.7166 mL
40 mM 0.1115 mL 0.5575 mL 1.1150 mL 2.7874 mL
50 mM 0.0892 mL 0.4460 mL 0.8920 mL 2.2300 mL
60 mM 0.0743 mL 0.3717 mL 0.7433 mL 1.8583 mL
80 mM 0.0557 mL 0.2787 mL 0.5575 mL 1.3937 mL
100 mM 0.0446 mL 0.2230 mL 0.4460 mL 1.1150 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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Etofylline 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:

Etofylline519-37-97-(β-Hydroxyethyl)theophyllinePhosphodiesterase (PDE)OralBronchodilatorAnti-inflammatoryInhibitorinhibitorinhibit

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