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Doxazosin mesylate

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Chemical Structure| 77883-43-3 同义名 : UK 33274 mesylate;Doxazosin (mesylate);UK 33274-27
CAS号 : 77883-43-3
货号 : A567154
分子式 : C24H29N5O8S
纯度 : 98%
分子量 : 547.581
MDL号 : MFCD00216023
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(63.92 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(1.83 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • α-adrenergic receptor
描述 Doxazosin mesylate is a selective alpha 1-inhibitor used as an antihypertensive agent[3]. Doxazosin, at concentrations of 5-20 mumol/L, increased LDL(low-density lipoproteins) 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[4]. Further, doxazosin(25 μmol/L) exerts its apoptotic effects against benign and malignant prostate cells via a death receptor–mediated mechanism with a potential integrin contribution towards cell survival outcomes[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00285519 Hypertension Phase 4 Completed - Japan ... 展开 >> Division of Cardiovascular Medicine, Department of Medicine, Jichi Medical University School of Medicine Shimotsuke, Tochigi, Japan, 329-0498 收起 <<
NCT00295542 Hypertension Phase 4 Completed - Spain ... 展开 >> Hospital Clinico Universitario Santiago de Compostela, Spain, 15706 收起 <<
NCT00741585 Essential Hypertension ... 展开 >> Cardiovascular Disease Stroke Chronic Kidney Disease 收起 << Phase 4 Completed - Spain ... 展开 >> CS Friol Friol, Lugo, Spain, 27220 CS Baiona Baiona, Pontevedra, Spain, 36300 CS Bueu Bueu, Pontevedra, Spain, 36930 CS A Estrada La Estrada, Pontevedra, Spain, 26680 CS A Guarda La Guardia, Pontevedra, Spain, 36780 CS Valmiñor Nigran, Pontevedra, Spain, 36250 CS Panxón Nigrán, Pontevedra, Spain, 36340 CS Tomiño Tomiño, Pontevedra, Spain, 36200 Bioengineering & Chronobilogy Labs., University of Vigo Vigo, Pontevedra, Spain, 36200 Hospital do Meixoeiro Vigo, Pontevedra, Spain, 36200 CS Calle Cuba Vigo, Pontevedra, Spain, 36202 CS A Doblada Vigo, Pontevedra, Spain, 36205 CS Coia Vigo, Pontevedra, Spain, 36209 CS Sardoma Vigo, Pontevedra, Spain, 36214 CS Teis Vigo, Pontevedra, Spain, 36216 CS Vilaboa Vilaboa, Pontevedra, Spain, 36141 CS San Roque Vilagarcía De Arousa, Pontevedra, Spain, 36600 CS Fingoi Lugo, Spain, 27002 Complexo Hospitalario Universitario de Ourense Orense, Spain, 32005 CS Lerez Pontevedra, Spain, 36156 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.13mL

1.83mL

0.91mL

18.26mL

3.65mL

1.83mL
参考文献

[1]Garrison JB, Kyprianou N. Doxazosin induces apoptosis of benign and malignant prostate cells via a death receptor-mediated pathway. Cancer Res. 2006 Jan 1;66(1):464-72.

[2]Kowala MC, Nunnari JJ, et al. Doxazosin and cholestyramine similarly decrease fatty streak formation in the aortic arch of hyperlipidemic hamsters. Atherosclerosis. 1991 Nov;91(1-2):35-49.

[3]Dhanya B, Suganthi A, Sen AK, Sahoo U, Seth AK. Determination of Doxazosin Mesylate in Tablets by RP-HPLC. Indian J Pharm Sci. 2011 Jan;73(1):120-2. doi: 10.4103/0250-474X.89772. PMID: 22131637; PMCID: PMC3224404.

[4]D'Eletto RD, Javitt NB. Effect of doxazosin on cholesterol synthesis in cell culture. J Cardiovasc Pharmacol. 1989;13 Suppl 2:S1-4; discussion S4. doi: 10.1097/00005344-198900132-00002. PMID: 2471008.

[5]Garrison JB, Kyprianou N. Doxazosin induces apoptosis of benign and malignant prostate cells via a death receptor-mediated pathway. Cancer Res. 2006 Jan 1;66(1):464-72. doi: 10.1158/0008-5472.CAN-05-2039. PMID: 16397262; PMCID: PMC1850148.