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    Doxazosin Mesylate (UK 33274 mesylate)
    Doxazosin Mesylate (UK 33274 mesylate)

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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 #: V1096
    CAS #: 77883-43-3Purity ≥98%

    Description: Doxazosin mesylate (formerly UK-33274; UK 33274; trade names Cardura), the mesylate salt of Doxazosin which is a quinazoline-derivative, is a potent and selective antagonist of postsynaptic α1-adrenergic receptors (so called alpha-blockers) with anti-hypertensive effects. It has been approved for use in the treatment of high blood pressure and urinary retention associated with benign prostatic hyperplasia. Doxazosin inhibits the binding of norepinephrine, which is released from sympathetic nerve terminals, to the α-1 receptors on the membrane of vascular smooth muscle cells. Doxazosin nt also shows high affinity to alpha-1c adrenoceptor, the predominant functional type in the prostate, which may partially attribute to its effect in treatment of benign prostatic hyperplasia. 

    References: Cancer Res. 2006 Jan 1;66(1):464-72; Atherosclerosis. 1991 Nov;91(1-2):35-49.

    Related CAS: 74191-85-8 (free base); 1126848-44-9 (Doxazosin D8)

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    • 香港大学
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    Molecular Weight (MW)547.58
    FormulaC23H25N5O5.CH4O3S 
    CAS No.77883-43-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 15 mg/mL (27.4 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: (4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanone methanesulfonate

    InChi Key: VJECBOKJABCYMF-UHFFFAOYSA-N

    InChi Code: InChI=1S/C23H25N5O5.CH4O3S/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20;1-5(2,3)4/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26);1H3,(H,2,3,4)

    SMILES Code: O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4COC5=CC=CC=C5O4.OS(=O)(C)=O

    SynonymsUK-33274 mesylate; UK33274 mesylate; UK 33274 mesylate 


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    In Vitro

    In vitro activity: Doxazosin-induced apoptosis is blocked by specific caspase-8 inhibitors, supporting the functional involvement of caspase-8 in doxazosin-induced apoptosis. Doxazosin increases FADD recruitment and subsequent caspase-8 activation, implicating Fas-mediated apoptosis as the underlying mechanism of the effect of Doxazosin in prostate cells. Doxazosin and cholestyramine similarly decreases plasma total and LDL plus VLDL cholesterols, and total triglycerides on average by 46%, 61% and 45% respectively. Doxazosin induces DNA damage and cell death in HL-1 cell line. Doxazosin treatment decreases cell viability in primary cultures of neonatal rat cardiomyocytes, and Hoechst dye vital staining demonstrates doxazosin-induced apoptosis in primary cultures of human adult cardiomyocytes. Doxazosin antagonizes the VEGF-mediated angiogenic response of HUVEC cells, by abrogating cell adhesion to fibronectin and collagen-coated surfaces and inhibiting cell migration, via a potential downregulation of VEGF expression. 

    In VivoDoxazosin also reduces mean arterial pressure by 18% without affecting heart rate in all hamsters. Doxazosin causes a significant reduction in the wet weight of BabeTGF-beta 1-infected mouse prostate reconstitution (MPR).  
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    References

    Cancer Res. 2006 Jan 1;66(1):464-72; Atherosclerosis. 1991 Nov;91(1-2):35-49; Prostate. 1997 Nov 1;33(3):157-63.


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

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