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甲磺酸多沙唑嗪 /Doxazosin mesylate {[allProObj[0].p_purity_real_show]}

货号:A567154 同义名: UK 33274 mesylate;Doxazosin (mesylate)

Doxazosin mesylate is a selective α1-adrenergic receptor blocker, used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Doxazosin mesylate 化学结构 CAS号:77883-43-3
Doxazosin mesylate 化学结构
CAS号:77883-43-3
Doxazosin mesylate 3D分子结构
CAS号:77883-43-3
Doxazosin mesylate 化学结构 CAS号:77883-43-3
Doxazosin mesylate 3D分子结构 CAS号:77883-43-3
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Doxazosin mesylate 纯度/质量文件 产品仅供科研

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α1D-adrenoceptor, pKi: 5.1

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β1-adrenoceptor, pIC50: 5.1

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adrenoceptor α2A, pKi: 7.1

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Prazosin HCl 95%
Silodosin 98%
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Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

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Doxazosin mesylate 98%
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β2-adrenergic receptor, Ki: 0.7nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Doxazosin mesylate 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].

Doxazosin mesylate 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 <<

Doxazosin mesylate 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.

Doxazosin mesylate 实验方案

计算器
存储液制备 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

Doxazosin mesylate 技术信息

CAS号77883-43-3
分子式C24H29N5O8S
分子量 547.581
别名 UK 33274 mesylate;Doxazosin (mesylate);UK 33274-27
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

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
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