product name Doxofylline
Description: Doxofylline, also known as Ansimar and ABC-12-3, is a novel phosphodiesterase inhibitor and a xanthine derivative drug for asthma. Doxofyllines mechanism of action is related to the inhibition of phosphodiesterase activities, but it appears to have decreased affinities towards adenosine A1 and A2 receptors, which may account for its better safety profile.
References: Expert Opin Pharmacother. 2009 Oct;10(14):2343-56; Curr Med Res Opin. 2001;16(4):258-68.
266.25
Formula
C11H14N4O4
CAS No.
69975-86-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 53 mg/mL (199.1 mM)
Solubility (In vivo)
Synonyms
Doxophylline
other peoduct :
| In Vitro |
In vitro activity: Doxofylline has PDE inhibitor activity and can increase the level of cAMP, which could, therefore, be used for the treatment of asthma and COPD. EC50 value of Doxofylline is 15 times higher than that of aminophylline in inhibiting the adenosine-induced relaxation of tracheal smooth muscle and 10 times higher in reducing the negative inotropic effect induced by adenosine on isolated guinea-pig atria. Doxofylline could effectively decrease the open probability of the calcium-activated potassium channels as a result of both the shortening of open period and the prolongation of close time. Doxofylline has greatly decreased affinity towards adenosine A1 and A2 receptors when compared with theophylline, which may contribute to the better safety profile. Moreover, unlike theophylline, Doxofylline does not interfere with calcium influx into cells nor antagonizes the action of calcium-channel blockers. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Doxofylline has been shown to have better efficacy with fewer side effects than theophylline. 30 mg/kg Doxofylline increases heart rate of anaesthetized cat by 13 beats/min. The effective therapeutic dose of Doxofylline has less cardio-stimulant effects than Theophylline, such that Doxofylline does not out significantly increase the cardiac frequency nor does it have arrhythmogenic effects. |
| Animal model | |
| Formulation & Dosage | |
| References | Expert Opin Pharmacother. 2009 Oct;10(14):2343-56; Curr Med Res Opin. 2001;16(4):258-68. |
