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

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

Phenoxybenzamine HCl 是一种非选择性的不可逆 α-肾上腺素受体拮抗剂,常用于研究嗜铬细胞瘤引起的高血压。Phenoxybenzamine HCl也具有抗肿瘤活性

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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+
Phenoxybenzamine HCl/盐酸酚苄明 化学结构 CAS号:63-92-3
Phenoxybenzamine HCl/盐酸酚苄明 化学结构
CAS号:63-92-3
Phenoxybenzamine HCl/盐酸酚苄明 3D分子结构
CAS号:63-92-3
Phenoxybenzamine HCl/盐酸酚苄明 化学结构 CAS号:63-92-3
Phenoxybenzamine HCl/盐酸酚苄明 3D分子结构 CAS号:63-92-3
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Phenoxybenzamine HCl/盐酸酚苄明 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 HCl 98%
Cisatracurium besylate 96%
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 α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

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

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 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 ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

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。

Phenoxybenzamine HCl/盐酸酚苄明 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/盐酸酚苄明 细胞实验

Cell Line
Concentration Treated Time Description References
Rat hippocampal slice cultures 0.1 µM–1 mM 24 hours To evaluate the neuroprotective effect of Phenoxybenzamine under oxygen glucose deprivation (OGD) conditions. Results showed that Phenoxybenzamine significantly reduced neuronal death induced by OGD over a broad dose range (0.1 µM–1 mM). Int J Mol Sci. 2014 Jan 20;15(1):1402-17

Phenoxybenzamine HCl/盐酸酚苄明 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Lateral fluid percussion (LFP) model of severe traumatic brain injury Intravenous injection 1 mg/kg Single administration, 8 hours post-injury To evaluate the neuroprotective effect of Phenoxybenzamine after severe traumatic brain injury. Results showed that Phenoxybenzamine significantly improved neurological severity scores and foot fault assessments, and at 25 days post-injury, it significantly improved learning and memory compared to saline-treated controls. Additionally, Phenoxybenzamine-treated animals had significantly lower expression of pro-inflammatory signaling proteins CCL2, IL1β, and MyD88 at 32 hours post-TBI. Int J Mol Sci. 2014 Jan 20;15(1):1402-17

Phenoxybenzamine HCl/盐酸酚苄明 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/盐酸酚苄明 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/盐酸酚苄明 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/盐酸酚苄明 技术信息

CAS号63-92-3
分子式C18H23Cl2NO
分子量 340.29
SMILES Code CC(N(CC1=CC=CC=C1)CCCl)COC2=CC=CC=C2.[H]Cl
MDL No. MFCD00055152
别名 Phenoxybenzamine (hydrochloride); NSC 37448; NCI-c01661; Phenoxybenzamine hydrochloride
运输蓝冰
InChI Key VBCPVIWPDJVHAN-UHFFFAOYSA-N
Pubchem ID 5284441
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

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

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
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