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/ Doxazosin mesylate/甲磺酸多沙唑嗪

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

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

Doxazosin mesylate 是一种选择性 α₁-肾上腺素能受体拮抗剂，常用于高血压及良性前列腺增生（BPH）相关尿潴留的研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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/甲磺酸多沙唑嗪 化学结构 CAS号：77883-43-3
Doxazosin mesylate/甲磺酸多沙唑嗪 化学结构
CAS号：77883-43-3
Doxazosin mesylate/甲磺酸多沙唑嗪 3D分子结构
CAS号：77883-43-3
Doxazosin mesylate/甲磺酸多沙唑嗪 化学结构 CAS号：77883-43-3
Doxazosin mesylate/甲磺酸多沙唑嗪 3D分子结构 CAS号：77883-43-3
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Doxazosin mesylate/甲磺酸多沙唑嗪 纯度/质量文件 产品仅供科研

货号：A567154 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ 98%
Maprotiline HCl ✔ 98%
Cisatracurium besylate ✔ 96%
Yohimbine HCI ✔ 99+%
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

 		+

β1-adrenoceptor, pIC50: 5.1

 		97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

 		97%
Piribedil ++

adrenoceptor α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

 		98%
Prazosin HCl ✔ 95%
Silodosin ✔ 98%
Phenoxybenzamine HCl ✔ 98%
Labetalol HCl ✔ 98+%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

 		98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		99%
Alfuzosin HCl ✔ 98%
Terazosin HCl ✔ 99%
Atipamezole ✔ 95%
Phentolamine methanesulfonate salt ✔ 99%
Carvedilol ✔ 99%
Doxazosin mesylate ✔ 99%
Tolazoline HCl ✔ 98%
Esmolol HCl ✔ 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

 		99%
Zenidolol HCl ++++

β2-adrenergic receptor, Ki: 0.7nM

β1-adrenergic receptor, Ki: 611nM

 		98%
Acebutolol HCl ✔ 97+%
Carteolol HCl ✔ 98+%
Betaxolol ✔ 99%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

 		97%
Bisoprolol ✔ 97%
Sotalol HCl ✔ 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

 		99%
Metoprolol ✔ 98+%
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/甲磺酸多沙唑嗪 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/甲磺酸多沙唑嗪 细胞实验

Cell Line
Concentration Treated Time Description References
U3118shBMI1 5 µM 8 days To evaluate the effect of Doxazosin on the proliferation of U3118shBMI1 cells, results showed that Doxazosin had no significant effect on the proliferation of U3118shBMI1 cells Oncogene. 2020 Mar;39(12):2523-2538.
U3118shScr 5 µM 8 days To evaluate the effect of Doxazosin on the proliferation of U3118shScr cells, results showed that Doxazosin significantly inhibited the proliferation of U3118shScr cells Oncogene. 2020 Mar;39(12):2523-2538.
HL-1 cells 17.3 μM (EC50) 19.5 hours To study doxazosin-induced apoptosis in HL-1 cells, results showed that doxazosin induced apoptosis by enhancing EphA2 phosphorylation (2.2-fold), activating pro-apoptotic downstream factors (e.g., phospho-SHP-2, phospho-p38 MAPK, and GADD153), and leading to caspase 3 cleavage. Br J Pharmacol. 2012 Dec;167(7):1563-72.
LX-2 cells 10 μM 6, 12, 24 hours Doxazosin significantly decreased HSC migration. Drug Des Devel Ther. 2021 Aug 21;15:3643-3659.
LX-2 cells 1, 5, 10, 20, 30, 40, 50, 60 μM 24 hours Doxazosin significantly inhibited LX-2 cell proliferation in a concentration-dependent manner, with an IC50 of 30.69 μmol/L. Drug Des Devel Ther. 2021 Aug 21;15:3643-3659.
PC3 cells 100 μM 1 hour To evaluate the antagonistic effect of EM2 on EphA2 phosphorylation. Results showed that EM2 significantly reduced doxazosin-induced EphA2 phosphorylation and prevented cell rounding. Sci Rep. 2017 May 15;7(1):1881.

Doxazosin mesylate/甲磺酸多沙唑嗪 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Stargardt disease model mice Intraperitoneal injection 1 mg/kg, 2 mg/kg, 3 mg/kg, 10 mg/kg Single dose, 30 minutes before light exposure Evaluate the protective effect of α1-AR antagonists on bright light-induced retinopathy, results showed DOX significantly protected retinal morphology and function J Clin Invest. 2013 Dec;123(12):5119-34
NODSCID mice U3118 xenograft model Subcutaneous injection 100 mg/kg Daily for 16 weeks To evaluate the effect of Doxazosin on U3118shScr and U3118shBMI1 xenograft tumors, results showed that Doxazosin significantly reduced the volume and proliferation of U3118shScr tumors, but had no significant effect on U3118shBMI1 tumors Oncogene. 2020 Mar;39(12):2523-2538.
CD-1 mice Paracetamol-induced hepatotoxicity model Intraperitoneal injection 35.7 mmol/kg Single dose, 1 hour before paracetamol To evaluate the protective effect of doxazosin against paracetamol-induced hepatotoxicity. Results showed that doxazosin significantly reduced serum ALT activity, indicating hepatoprotective effects. Br J Pharmacol. 2008 Feb;153(4):820-30
C57BL/6 mice Carbon tetrachloride (CCl4)-induced mouse liver fibrosis model Gavage 2.5, 5, 10 mg/(kg*day) Once daily for 20 weeks Doxazosin improved the survival rates of CCl4-induced mice and alleviated pathological damage associated with liver fibrosis. Drug Des Devel Ther. 2021 Aug 21;15:3643-3659.
Zebrafish larvae Adgrl3.1 mutant model System water 0.1 µM, 1 µM, 10 µM, 30 µM, 100 µM Single administration, 1 hour before recording To evaluate the rescue effect of Doxazosin on the hyperactive phenotype of adgrl3.1 mutant zebrafish larvae. Results showed that all tested doses significantly reduced the average distance moved in mutant larvae. Neuropsychopharmacology. 2023 Jul;48(8):1155-1163

Doxazosin mesylate/甲磺酸多沙唑嗪 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/甲磺酸多沙唑嗪 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/甲磺酸多沙唑嗪 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/甲磺酸多沙唑嗪 技术信息

CAS号77883-43-3
分子式C24H29N5O8S
分子量 547.58
SMILES Code O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4OC5=CC=CC=C5OC4.CS(=O)(O)=O
MDL No. MFCD00216023
别名 UK 33274 mesylate; Doxazosin (mesylate); UK 33274-27
运输蓝冰
InChI Key VJECBOKJABCYMF-UHFFFAOYSA-N
Pubchem ID 62978
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Doxazosin | 77883-43-3 | UK 33274 | UK33274 | UK-33274 | Autophagy Inducer | GPCR/G Protein | Neuronal Signaling | Autophagy | Adrenergic Receptor | Autophagy | Mitophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Doxazosin mesylate/甲磺酸多沙唑嗪 纯度/质量文件 | Doxazosin mesylate/甲磺酸多沙唑嗪 亚型比较 | Doxazosin mesylate/甲磺酸多沙唑嗪 生物活性 | Doxazosin mesylate/甲磺酸多沙唑嗪 临床数据 | Doxazosin mesylate/甲磺酸多沙唑嗪 参考文献 | Doxazosin mesylate/甲磺酸多沙唑嗪 实验方案 | Doxazosin mesylate/甲磺酸多沙唑嗪 技术信息

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