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Doxazosin

Catalog No. T22316   CAS 74191-85-8
Synonyms: UK 33274

Doxazosin (UK 33274) is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms.

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Doxazosin Chemical Structure
Doxazosin, CAS 74191-85-8
Pack Size Availability Price/USD Quantity
5 mg In stock $ 40.00
10 mg In stock $ 57.00
25 mg In stock $ 94.00
50 mg In stock $ 138.00
100 mg In stock $ 209.00
200 mg In stock $ 325.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.85%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Doxazosin (UK 33274) is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms.
In vitro Doxazosin, at concentrations of 5-20 mumol/L, increased LDL binding to hepatic cells in a dose-related manner. Also, in these hepatic cells, doxazosin produced dose-related decreases in both newly synthesized cholesterol and cholesterol ester. In rabbit fibroblasts that were LDL receptor negative, de novo cholesterol synthesis was markedly reduced by increasing concentrations of doxazosin. Taken together, these results suggest that doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor[2].
In vivo Both the enantiomers were highly bound to the plasma proteins of rats, dogs and humans [(-)doxazosin: 89.4%-94.3%; (+)doxazosin: 90.9%-95.4%]. (+)Doxazosin exhibited significantly higher protein binding capacities than (-)doxazosin in all the three species, and the difference in the bound concentration (Cb) between the two enantiomers was enhanced as their concentrations were increased. Although the percentage of the plasma protein binding in the dog plasma was significantly lower than that in the human plasma at 400 and 800 ng/mL, the corrected percentage of plasma protein binding was dog>human>rat[3].
Synonyms UK 33274
Molecular Weight 451.48
Formula C23H25N5O5
CAS No. 74191-85-8

Storage

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

Solubility Information

DMSO: 27.5 mg/ml (60.91 mM)

TargetMolReferences and Literature

1. Miura, Y. and K. Yoshinaga, Doxazosin: a newly developed, selective alpha 1-inhibitor in the management of patients with pheochromocytoma. Am Heart J, 1988. 116(6 Pt 2): p. 1785-9. 2. D'Eletto, R.D. and N.B. Javitt, Effect of doxazosin on cholesterol synthesis in cell culture. J Cardiovasc Pharmacol, 1989. 13 Suppl 2: p. S1-4; discussion S4. 3. Sun, J.A., et al., Stereoselective binding of doxazosin enantiomers to plasma proteins from rats, dogs and humans in vitro. Acta Pharmacol Sin, 2013. 34(12): p. 1568-74.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Anti-Cardiovascular Disease Compound Library Drug Repurposing Compound Library Orally Active Compound Library ReFRAME Related Library Approved Drug Library Human Metabolite Library

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Keywords

Doxazosin 74191-85-8 GPCR/G Protein Neuroscience Adrenergic Receptor inhibit UK33274 Inhibitor Beta Receptor UK 33274 UK-33274 inhibitor

 

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