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    Doxofylline
    Doxofylline

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0794
    CAS #: 69975-86-6Purity ≥98%

    Description: Doxofylline (also known as Neothylline; Ansimar; ABC-1213; ALT-07; Lufyllin; DO-309; Diprophylline; Corphyllin; ABC-12-3), a xanthine derivative, is a novel and potent PDE (phosphodiesterase) inhibitor with the potential for treating asthma. Doxofylline's 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.

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    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


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    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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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