GRADE & PURITY 10mM in DMSO

Synonyms

Methanone, [4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl](2,3-dihydro-1,4-benzodioxin-2-yl)-, methanesulfonate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Doxazosin, a quinazoline-derivative, selectively antagonizes postsynapticα1-adrenergic receptors, used in the treatment of high blood pressure and urinary retention associated with benign prostatic hyperplasia.
In vitro

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 vivo

Doxazosin 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).
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

Methanone, [4-(4-amino-6, 7-dimethoxy-2-quinazolinyl)-1-piperazinyl](2, 3-dihydro-1, 4-benzodioxin-2-yl)-, methanesulfonate

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Doxazosin, a quinazoline-derivative, selectively antagonizes postsynaptic α1-adrenergic receptors, used in the treatment of high blood pressure and urinary retention associated with benign prostatic hyperplasia.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

ANTAGONIST

Mecanismo de acción

Adrenergic receptor alpha-1 antagonist

Nombres e identificadores

• Isómeros SMILES: COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4COC5=CC=CC=C5O4)N)OC.CS(=O)(=O)O
• WGK Alemania: 2
• Peso molecular: 547.58
• Reaxy-Rn: 7791129
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7791129&ln=

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: Insoluble; Water: Insoluble; Ethanol: Insoluble
• Punto de fusión (°C): 269 °C

Referencias

1. Hao Gu, Kang Ma, Weiqian Zhao, Lirong Qiu, Wei Xu.  (2021)  A general purpose MALDI matrix for the analyses of small organic, peptide and protein molecules.  ANALYST,  146  (12): (4080-4086).  [PMID:34052846] [10.1039/D1AN00474C]