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盐酸酚苄明 /Phenoxybenzamine HCl {[allProObj[0].p_purity_real_show]}

货号:A398762 同义名: Phenoxybenzamine (hydrochloride);NSC 37448

Phenoxybenzamine HCl is a non-selective irreversible dibenzamine α adrenergic antagonist with antihypertensive and vasodilatory properties.

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Type HazMat fee for 500 gram (Estimated)
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Phenoxybenzamine HCl 化学结构 CAS号:63-92-3
Phenoxybenzamine HCl 化学结构
CAS号:63-92-3
Phenoxybenzamine HCl 3D分子结构
CAS号:63-92-3
Phenoxybenzamine HCl 化学结构 CAS号:63-92-3
Phenoxybenzamine HCl 3D分子结构 CAS号:63-92-3
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Phenoxybenzamine HCl 纯度/质量文件 产品仅供科研

货号:A398762 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 hydrochloride 98%
Cisatracurium besylate 98%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine 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

97%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Doxazosin mesylate 98%
Tolazoline HCl 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

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。

Phenoxybenzamine HCl 生物活性

靶点
  • α-adrenergic receptor

描述 Phenoxybenzamine hydrochloride is a selective antagonist of both α-adrenoceptor and calmodulin that is commonly used for the treatment of hypertension, specifically caused by pheochromocytoma. The IC50 (100 nM) derived from the blockade of [3H]yohimbine binding by phenoxybenzamine was significantly less than the IC50 (550 nM) for the corresponding reversal by phenoxybenzamine of the effects of norepinephrine on cyclic AMP accumulation[2]. Phenoxybenzamine hydrochloride (50 nM) in conbination with Phenoxybenzamine hydrochloridetolamine (1000 nM) enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with pretreatment with Phenoxybenzamine hydrochloride (50 nM) alone in endothelium-intact aortae. Combined treatment with either dexmedetomidine (300 or 1000 nM) and Phenoxybenzamine hydrochloride (50 nM) or Phenoxybenzamine hydrochloridetolamine (1000 nM) and Phenoxybenzamine hydrochloride (50 nM) enhance Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with Phenoxybenzamine hydrochloride alone (50 nM)[3]. PHEN (Phenoxybenzamine Hydrochloride) exhibited a significant inhibitory effect on the proliferation of both U251 and U87MG glioma cell lines in a positive dose-dependent manner. PHEN apparently attenuated the malignancy of glioma in terms of migration and invasion and also suppressed the tumorigenic capacity both in vitro and in vivo[4].

Phenoxybenzamine HCl 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
NCT03176693 Pheochromocytoma ... 展开 >> Paraganglioma 收起 << Phase 3 Recruiting May 2024 United States, California ... 展开 >> University of California, Los angeles Recruiting Los Angeles, California, United States, 90025 Principal Investigator: Masha J Livhits, MD          Sub-Investigator: Eric J Kuo, MD 收起 <<
NCT00569855 - Completed - -
NCT00569855 Open-heart Surgery ... 展开 >> Cardiopulmonary Bypass 收起 << Phase 2 Completed - United States, Arkansas ... 展开 >> Arkansas Children's Hospital Little Rock, Arkansas, United States, 72207 收起 <<

Phenoxybenzamine HCl 参考文献

[1]Byon HJ, Ok SH, et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenoceptor Blockade and Nitric Oxide Release in Isolated Rat Aortae. Int J Med Sci. 2017 Feb 7;14(2):143-149.

[2]Lenox RH, Ellis J, Van Riper D, Ehrlich YH. Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve. Mol Pharmacol. 1985;27(1):1-9

[3]Byon HJ, Ok SH, Lee SH, et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenoceptor Blockade and Nitric Oxide Release in Isolated Rat Aortae. Int J Med Sci. 2017;14(2):143-149. Published 2017 Feb 7

[4]Lin XB, Jiang L, Ding MH, et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016;37(3):2901-2908

Phenoxybenzamine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.69mL

2.94mL

1.47mL

29.39mL

5.88mL

2.94mL

Phenoxybenzamine HCl 技术信息

CAS号63-92-3
分子式C18H23Cl2NO
分子量 340.287
别名 Phenoxybenzamine (hydrochloride);NSC 37448;NCI-c01661;Phenoxybenzamine hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 105 mg/mL(308.56 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

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