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Doxazosin mesylate

Catalog No. T0101 CAS 77883-43-3

Synonyms: UK 33274 mesylate

Doxazosin mesylate (UK 33274 mesylate)(UK 33274) is a quinazoline-derivative. It is a selectively antagonizes postsynaptic α1-adrenergic receptors.

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Doxazosin mesylate, CAS 77883-43-3

Pack Size	Availability	Price/USD
200 mg	In stock	$ 38.00
500 mg	In stock	$ 64.00
1 g	In stock	$ 82.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.98%

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Description	Doxazosin mesylate (UK 33274 mesylate)(UK 33274) is a quinazoline-derivative. It is a selectively antagonizes postsynaptic α1-adrenergic receptors.
In vitro	Doxazosin reduces mean arterial pressure by 18% without affecting the heart rate in all hamsters. It also significantly decreases the wet weight of mouse prostate reconstitution (MPR) in Beta TGF-β1-infected mice.
In vivo	Doxazosin, similar to chenodeoxycholic acid, decreases plasma total cholesterol, LDL plus VLDL cholesterol, and mean total triglycerides by 46%, 61%, and 45%, respectively. It diminishes the viability of neonatal rat cardiomyocytes in primary culture, with Hoechst staining in vivo indicating apoptosis in human-derived cardiomyocytes induced by Doxazosin. It prompts DNA damage and cell death in the HL-1 cell line. The apoptosis induced by Doxazosin can be blocked by a specific caspase-8 inhibitor, suggesting caspase-8’s functional involvement in the cell apoptosis triggered by Doxazosin. Moreover, Doxazosin antagonizes the VEGF-mediated angiogenic response in HUVEC cells by obliterating cell adhesion to fibronectin and collagen surfaces, and by inhibiting cell migration through downregulation of Vascular Endothelial Growth Factor expression. Doxazosin also increases FADD recruitment and caspase-8 activation, implying Fas-mediated apoptosis as a fundamental mechanism of Doxazosin's action in prostate cells.
Kinase Assay	Protease assays: To determine the inhibition constants (Ki) for each Prt inhibitor, purified HIV-1 RF wild-type Prt (2.5 nM) is incubated at 37 ℃ with 1 μM to 15 μM fluorogenic substrate in reaction buffer (1 M NaCl, 1 mM EDTA, 0.1 M sodium acetate [pH 5.5], 0.1% polyethylene glycol 8000) in the presence or absence of Atazanavir. Cleavage of the substrate is quantified by measuring an increase in fluorescent emission at 490 nM after excitation at 340 nM using a Cytofluor 4000. Reactions are carried out using 1.36 μM, 1.66 μM, 2.1 μM, 3.0 μM, 5.0 μM, or 15 μM substrate in the presence of five concentrations of Atazanavir (1.25 nM to 25 nM). Substrate cleavage is monitored at 5-min intervals for 30 min. Cleavage rates are then determined for each sample at early time points in the reaction, and Ki values are determined from the slopes of the resulting Michaelis-Menten plots.

Synonyms	UK 33274 mesylate
Molecular Weight	547.58
Formula	C24H29N5O8S
CAS No.	77883-43-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41.1 mg/mL (75 mM)

References and Literature

1. Garrison JB, et al. Cancer Res, 2006, 66(1), 464-472. 2. Kowala MC, et al. Atherosclerosis, 1991, 91(1-2), 35-49. 3. González-Juanatey JR, et al. Circulation. 2003 Jan 7;107(1):127-31. 4. Keledjian K, et al. J Cell Biochem, 2005, 94(2), 374-388. 5. Yang G, et al. Prostate, 1997, 33(3), 157-163.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Coagulation and Anticoagulation Compound Library FDA-Approved Drug Library Bioactive Compound Library Drug Metabolite/Impurity Library NO PAINS Compound Library

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Keywords

Doxazosin mesylate 77883-43-3 Autophagy GPCR/G Protein Neuroscience Mitophagy Adrenergic Receptor Mitochondrial Autophagy Beta Receptor UK-33274 Mesylate Doxazosin Inhibitor UK 33274 Mesylate UK-33274 UK 33274 mesylate UK 33274 UK33274 inhibit Doxazosin Mesylate UK33274 Mesylate inhibitor

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