1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Doxazosin

Doxazosin  (Synonyms: 多沙唑嗪; UK 33274)

目录号: HY-B0098 纯度: 99.85%
COA 产品使用指南

Doxazosin (UK 33274) 能选择性拮抗突触后的 α1 肾上腺素受体。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Doxazosin Chemical Structure

Doxazosin Chemical Structure

CAS No. : 74191-85-8

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规格 价格 是否有货 数量
5 mg ¥280
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10 mg ¥400
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25 mg ¥720
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Other Forms of Doxazosin:

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Adrenergic Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

α1-adrenergic receptors[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 EC50
> 100 μM
Compound: doxazosin
Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
[PMID: 19719240]
DU-145 EC50
100 μM
Compound: doxazosin
Induction of apoptosis in human DU145 cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay
Induction of apoptosis in human DU145 cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay
[PMID: 19719240]
DU-145 IC50
30.56 μM
Compound: Doxazosin
Antiproliferative activity against human DU145 cells after 120 hrs by MTT assay
Antiproliferative activity against human DU145 cells after 120 hrs by MTT assay
[PMID: 28499171]
DU-145 IC50
37.44 μM
Compound: doxazosin
Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
[PMID: 19719240]
DU-145 IC50
37.67 μM
Compound: Doxazosin
Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay
Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay
[PMID: 25874333]
HEK293-A IC50
19 μM
Compound: doxazosin
Cytotoxicity against HEK293A cells transfected with alpha-1A adrenergic receptor assessed as cell viability by sulforhodamine B assay
Cytotoxicity against HEK293A cells transfected with alpha-1A adrenergic receptor assessed as cell viability by sulforhodamine B assay
[PMID: 26005522]
HEK293-A IC50
22 μM
Compound: doxazosin
Cytotoxicity against HEK293A cells transfected with alpha-1D adrenergic receptor assessed as cell viability by sulforhodamine B assay
Cytotoxicity against HEK293A cells transfected with alpha-1D adrenergic receptor assessed as cell viability by sulforhodamine B assay
[PMID: 26005522]
LNCaP IC50
10.48 μM
Compound: Doxazosin
Antiproliferative activity against human LNCAP cells after 120 hrs by MTT assay
Antiproliferative activity against human LNCAP cells after 120 hrs by MTT assay
[PMID: 28499171]
LNCaP EC50
100 μM
Compound: doxazosin
Induction of apoptosis in human LNCAP cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay
Induction of apoptosis in human LNCAP cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay
[PMID: 19719240]
LNCaP IC50
27.89 μM
Compound: Doxazosin
Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay
Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay
[PMID: 25874333]
LNCaP IC50
28.11 μM
Compound: doxazosin
Cytotoxicity against human LNCAP cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
Cytotoxicity against human LNCAP cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
[PMID: 19719240]
NHDF EC50
100 μM
Compound: doxazosin
Induction of apoptosis in human NHDF cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay
Induction of apoptosis in human NHDF cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay
[PMID: 19719240]
NHDF EC50
40.4 μM
Compound: doxazosin
Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
[PMID: 19719240]
NHDF IC50
43 μM
Compound: doxazosin
Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
[PMID: 19719240]
PC-3 EC50
> 100 μM
Compound: doxazosin
Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
[PMID: 19719240]
PC-3 IC50
> 50 μM
Compound: Doxazosin
Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay
Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay
[PMID: 25874333]
PC-3 EC50
100 μM
Compound: doxazosin
Induction of apoptosis in human PC3 cells assessed as caspase 3/7 activation after 24 hrs by Caspase-Glo 3/7 assay
Induction of apoptosis in human PC3 cells assessed as caspase 3/7 activation after 24 hrs by Caspase-Glo 3/7 assay
[PMID: 19719240]
PC-3 IC50
12.1 μM
Compound: Doxazosin
Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay
[PMID: 28499171]
PC-3 GI50
26.9 μM
Compound: Doxazosin
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
[PMID: 18817363]
PC-3 GI50
26.9 μM
Compound: Doxazosin
Cytotoxic activity on human PC3 prostate cancer cells by SRB assay
Cytotoxic activity on human PC3 prostate cancer cells by SRB assay
[PMID: 16302814]
PC-3 GI50
26.9 μM
Compound: Doxazosin
Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay
[PMID: 23252794]
PC-3 IC50
38.6 μM
Compound: doxazosin
Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay
[PMID: 19719240]
体外研究
(In Vitro)

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[1]. doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor. The inhibition of cholesterol synthesis by doxazosin may cause cells to compensate by upregulating the LDL receptor, thereby increasing the importation of lipoprotein cholesterol and reducing LDL cholesterol in the medium[2]. Doxazosin monotherapy was effective in eight of 12 patients (66.7%), and combined therapy with a beta-blocker was effective in 11 of 12 patients (91.7%). The mean pulse rate remained constant throughout therapy. Adverse reactions were minor and transient and occurred in only three patients. Urinary and plasma catecholamine levels tended to decrease or remained unchanged during doxazosin therapy[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

451.48

Formula

C23H25N5O5

CAS 号
性状

固体

颜色

White to off-white

中文名称

多沙唑嗪

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (221.49 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2149 mL 11.0747 mL 22.1494 mL
5 mM 0.4430 mL 2.2149 mL 4.4299 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.54 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.54 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2149 mL 11.0747 mL 22.1494 mL 55.3734 mL
5 mM 0.4430 mL 2.2149 mL 4.4299 mL 11.0747 mL
10 mM 0.2215 mL 1.1075 mL 2.2149 mL 5.5373 mL
15 mM 0.1477 mL 0.7383 mL 1.4766 mL 3.6916 mL
20 mM 0.1107 mL 0.5537 mL 1.1075 mL 2.7687 mL
25 mM 0.0886 mL 0.4430 mL 0.8860 mL 2.2149 mL
30 mM 0.0738 mL 0.3692 mL 0.7383 mL 1.8458 mL
40 mM 0.0554 mL 0.2769 mL 0.5537 mL 1.3843 mL
50 mM 0.0443 mL 0.2215 mL 0.4430 mL 1.1075 mL
60 mM 0.0369 mL 0.1846 mL 0.3692 mL 0.9229 mL
80 mM 0.0277 mL 0.1384 mL 0.2769 mL 0.6922 mL
100 mM 0.0221 mL 0.1107 mL 0.2215 mL 0.5537 mL
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HY-B0098
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