Cat. No.: HY-B1209

Etofylline

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

Customer Review

Based on 1 Customer Validation

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.

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

Purity: 99.72%
CAS No.: 519-37-9
Formula: C₉H₁₂N₄O₃
Molecular Weight:224.22

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Etofylline Chemical Structure

CAS No.: 519-37-9

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Biological Activity
- Description
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Phosphodiesterase (PDE) Isoforms :

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)	V_dβ	Cl(1/kg/h)	t_1/2 (h)	1/MRT_b(h^-14)	V_dss (1/kg)	MRT_b(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	C_max (ng/mL)	T_max (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.

Chemical Information

CAS No. 519-37-9
Appearance Solid
Molecular Weight 224.22
Formula C₉H₁₂N₄O₃
Color White to off-white
SMILES

O=C(N1C)N(C)C2=C(N(CCO)C=N2)C1=O
Synonyms

7-(β-Hydroxyethyl)theophylline
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 : 23.33 mg/mL (104.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.4599 mL

22.2995 mL

44.5991 mL

5 mM

0.8920 mL

4.4599 mL

8.9198 mL

10 mM

0.4460 mL

2.2300 mL

4.4599 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (11.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wattanaporn Tavipatana, et al.Etophylline and theophylline pharmacokinetics when administered concomitantly in rabbits. International Journal of Pharmaceutics. Volume 30, Issues 2–3

[2]. Chandrakantsing V Pardeshi ,et al. Mannose-anchored N,N,N-trimethyl chitosan nanoparticles for pulmonary administration of etofylline. Int J Biol Macromol. 2020 Dec 15;165(Pt A):445-459. [Content Brief]

[3]. Ram Manohar Basnet, et al. Zebrafish Embryo as an In Vivo Model for Behavioral and Pharmacological Characterization of Methylxanthine Drugs. Int J Mol Sci. 2017 Mar 9;18(3):596. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

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Anti-Cardiovascular Disease Compound Library

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Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

MCE Kinase Hinge Binder Fragment Library

All Phosphodiesterase (PDE) Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Etofylline

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

MCE Kinase Hinge Binder Fragment Library

All Phosphodiesterase (PDE) Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Etofylline Related Classifications

HY-B1209 Related Classifications