Doxofylline

SKU: orb1310571

Description

Doxofylline is a 7-dioxolane-substituted methylxanthine used in asthma research. It demonstrates bronchodilatory efficacy comparable to theophylline in both in vitro and in vivo studies, while exhibiting an improved safety profile with fewer adverse effects such as central nervous system stimulation.

Research Area

Immunology & Inflammation, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 69975-86-6
• MW: 266.25
• Purity: >99.99% (May vary between batches)
• Formula: C₁₁H₁₄N₄O₄
• SMILES: Cn1c2ncn(CC3OCCO3)c2c(=O)n(C)c1=O
• Target: PDE,ROS,Reactive Oxygen Species,Adenosine Receptor
• Solubility: DMSO:50 mg/mL (187.79 mM);H2O:22 mg/mL (82.63 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.51 mM);Ethanol:2 mg/mL (7.51 mM)

Bioactivity

• In Vivo:
  Doxofylline exhibits the activity of a phosphodiesterase (PDE) inhibitor and enhances the levels of cyclic adenosine monophosphate (cAMP), thus it is utilized in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Compared to theophylline, doxofylline significantly reduces the affinity for adenosine A1 and A2 receptors, which may contribute to its improved safety profile. Additionally, doxofylline does not interfere with calcium ion influx nor antagonize calcium channel blockers. In terms of inhibitory potency, the half-maximal effective concentration (EC50) of doxofylline against adenosine-induced tracheal smooth muscle relaxation is 15-fold higher than that of aminophylline, and it also displays a 15-fold higher EC50 in reducing the negative inotropic effect of adenosine on guinea pig atria than aminophylline.
• In Vitro:
  At an effective therapeutic dose, Doxofylline exhibits a less pronounced cardiac stimulant effect compared to theophylline. As a result, Doxofylline does not significantly increase heart rate, nor does it induce arrhythmias. Administration of 30 mg/kg of Doxofylline results in an increase of 13 beats/min in the heart rate of anesthetized cats.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

bronchospasm, bronchitis, BM cells, asthma, AdenosineReceptor, Adenosine Receptor, 16HBE cells, Doxofylline, Doxophylline, COPD, PDE, inhibit, Inhibitor, P1 receptor, phosphodiesterase, Phosphodiesterase (PDE), Reactive Oxygen Species

Compound Identifiers

PubChem CID

50942