| Name | Doxofylline |
| Description | Doxofylline (Doxophylline) is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has shown similar efficacy to theophylline but with significantly fewer side effects in animal and human studies. |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (187.79 mM)
H2O : 22 mg/mL (82.6 mM)
Ethanol : 2 mg/mL (7.51 mM)
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| Keywords | COPD | asthma | inhibit | Reactive Oxygen Species | Adenosine Receptor | bronchospasm | 16HBE cells | Inhibitor | BM cells | Phosphodiesterase (PDE) | Doxofylline | bronchitis | P1 receptor |
| Inhibitors Related | Theophylline monohydrate | Inosine | Theobromine | Apremilast | Indomethacin | Icariin | Theophylline |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Inflammatory Traditional Chinese Medicine Compound Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
