Doxazosin Mesylate

Catalog No.S1324 Batch:S132401

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Technical Data

Formula

C23H25N5O5.CH4O3S

Molecular Weight 547.58 CAS No. 77883-43-3
Solubility (25°C)* In vitro DMSO 27 mg/mL (49.3 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
α1-adrenergic receptor [1]
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. [1] Doxazosin and cholestyramine similarly decreases plasma total and LDL plus VLDL cholesterols, and total triglycerides on average by 46%, 61% and 45% respectively. [2] 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. [3] 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. [4]
In vivo Doxazosin also reduces mean arterial pressure by 18% without affecting heart rate in all hamsters. [2] Doxazosin causes a significant reduction in the wet weight of BabeTGF-beta 1-infected mouse prostate reconstitution (MPR). [5]

Protocol (from reference)

Customer Product Validation

Data from [J Clin Invest, 2013, 123(12), 5119-34]

Data from [Data independently produced by , , Prostate, 2016, 76(8):757-66]

Data from [Data independently produced by , , J Ocul Pharmacol Ther, 2017, 33(1):50-56]

Selleck's Doxazosin Mesylate has been cited by 5 publications

Suppression of TNBC metastasis by doxazosin, a novel dual inhibitor of c-MET/EGFR [ J Exp Clin Cancer Res, 2023, 10.1186/s13046-023-02866-z] PubMed: 37924112
Antiangiogenic Effects of Doxazosin on Experimental Choroidal Neovascularization in Mice. [Guo J, et al. J Ocul Pharmacol Ther, 2017, 33(1):50-56] PubMed: 27992238
Relative cytotoxic potencies and cell death mechanisms of α1 -adrenoceptor antagonists in prostate cancer cell lines [Forbes A, et al. Prostate, 2016, 76(8):757-66] PubMed: 26880388
Irbesartan, an FDA approved drug for hypertension and diabetic nephropathy, is a potent inhibitor for hepatitis B virus entry by disturbing Na+-dependent taurocholate cotransporting polypeptide activity [Wang XJ, et al. Antiviral Res, 2015, 120:140-6] PubMed: 26086883
Systems pharmacology identifies drug targets for Stargardt disease-associated retinal degeneration. [Chen Y, et al. J Clin Invest, 2013, 123(12):5119-34] PubMed: 24231350

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.