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Submit ReviewDoxazosin mesylate
说明： α1 antagonist
别名： UK 33274
化学名： 4-Amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazoline methanesulfonate
纯度： ≥99% (HPLC)
生物活性 for Doxazosin mesylate
Doxazosin mesylate is a selective α1-adrenoceptor antagonist (pKi values are 9.0, 8.5 and 8.4 for human α1B, α1A and α1D receptors respectively). Displays antihypertensive activity.
Scientific Data
Cell Viability
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Reduced viability of differentiated cardiomyocytes exposed to cardiotoxic small molecules. The viability of differentiated cardiomyocytes was assessed using a Resazurin metabolism assay. A) Untreated cells metabolize Resazurin (Catalog # AR002) to produce resorufin, a fluorescent molecule that can be measured using a fluorometric plate reader. Resorufin fluorescence accumulated in untreated cardiomyocytes. Cells treated with the cardiotoxic small molecules Staurosporine (blue; Catalog # 1285), a non-selective protein kinase inhibitor, or Doxazosin (tan; Catalog # 2964), an alpha 1 antagonist, did not metabolize Resazurin, as shown by lack of fluorescence accumulation, indicating a loss of viability upon treatment. B) Cell morphology of untreated, Staurosporine-treated, and Doxazosin-treated cardiomyocytes was assessed by brightfield microscopy.
化合物库 for Doxazosin mesylate
Doxazosin mesylate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Doxazosin mesylate
| 分子量 | 547.58 |
| 公式 | C23H25N5O5.CH3SO3H |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 77883-43-3 |
| PubChem ID | 62978 |
| InChI Key | VJECBOKJABCYMF-UHFFFAOYSA-N |
| Smiles | NC2=NC(N3CCN(C(C4COC(C=CC=C5)=C5O4)=O)CC3)=NC1=CC(OC)=C(OC)C=C12.CS(=O)(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Doxazosin mesylate
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 41.07 | 75 |
制备储备液 for Doxazosin mesylate
以下数据基于产品分子量 547.58。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 2.43 mL | 12.17 mL | 24.35 mL |
| 3.75 mM | 0.49 mL | 2.43 mL | 4.87 mL |
| 7.5 mM | 0.24 mL | 1.22 mL | 2.43 mL |
| 37.5 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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产品说明书 for Doxazosin mesylate
参考文献 for Doxazosin mesylate
参考文献是支持产品生物活性的出版物。
Alabaster and Davey (1986) The α1-adrenoceptor antagonist profile of doxazosin: preclinical pharmacology. Br.J.Clin.Pharmacol. 21 9S PMID: 2871857
Kenny et al (1996) Evaluation of the pharmacological selectivity profile of α1 adrenoceptor antagonists at prostatic α1 adrenoceptors: binding functional and in vivo studies. Br.J.Pharmacol. 118 871 PMID: 8799556
Ma et al (2006) Chiral selective effects of doxa. enantiomers on blood pressure and urinaruy bladder pressure in anesthetized rats. Acta Pharmacol.Sinica 27 1423 PMID: 17049117
If you know of a relevant reference for Doxazosin mesylate, please let us know.
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关键词: Doxazosin mesylate, Doxazosin mesylate supplier, α1-adrenoceptor, alpha1-adrenoceptor, a1-adrenergic, α1-adrenergic, alpha1-adrenergic, a1-adrenoceptor, antagonists, Receptors, UK33274, UK, 33274, Adrenergic, Alpha-1, 2964, Tocris Bioscience
4 篇 Doxazosin mesylate 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Doxazosin mesylate 的部分引用包括：
Kahn et al (2016) The anti-hypertensive drug pra. inhibits glioblastoma growth via the PKCδ-dependent inhibition of the AKT pathway. EMBO Mol Med 8 511 PMID: 27138566
Cilz et al (2014) DArgic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels. Cereb Cortex 24 3195 PMID: 23843440
Diaz et al (2014) Moderate Alcohol Exposure during the Rat Equivalent to the Third Trimester of Human Pregnancy Alters Regulation of GABAA Receptor-Mediated Synaptic Transmission by DA in the Basolateral Amygdala. Front Cell Neurosci 2 46 PMID: 24904907
Jahchan et al (2013) A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors. Cancer Discov 3 1364 PMID: 24078773
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Doxazosin mesylate 的评论
平均评分: 4 (Based on 1 Review.)
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Used to investigate cell metabolism.
By
Anonymous on 01/27/2023
分析类型： In Vitro
种属： Rat
细胞系/组织： Primary hippocampal neurons
The drug was incubated at 10 μM to investigate a potential effect on cell metabolism.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.