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Doxofylline
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Doxofylline图片
CAS NO:69975-86-6
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)266.25
FormulaC11H14N4O4
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)

Chemical Name: 7-((1,3-dioxolan-2-yl)methyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione

InChi Key: HWXIGFIVGWUZAO-UHFFFAOYSA-N

InChi Code: InChI=1S/C11H14N4O4/c1-13-9-8(10(16)14(2)11(13)17)15(6-12-9)5-7-18-3-4-19-7/h6-7H,3-5H2,1-2H3

SMILES Code: O=C(N1C)N(C)C2=C(N(CC3OCCO3)C=N2)C1=O

Synonyms

Doxofylline; Ansimar; ABC-1213; ALT-07; DO-309; Diprophylline; Lufyllin; Corphyllin; Neothylline; ABC 1213; ALT 07; DO 309; ABC1213; ALT07; DO309

实验参考方法
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.

In VivoDoxofylline 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 modelCats
Formulation & Dosage30 mg/kg
References

Expert Opin Pharmacother. 2009 Oct;10(14):2343-56; Curr Med Res Opin. 2001;16(4):258-68.