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

Phenoxybenzamine  (Synonyms: 酚苄明)

目录号: HY-B0431
产品使用指南

Phenoxybenzamine 是一种非选择性的、不可逆的、具有口服活性的 α-肾上腺素受体(α-adrenoceptor)拮抗剂,常用于研究嗜铬细胞瘤引起的高血压。 Phenoxybenzamine 也具有抗肿瘤活性。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Phenoxybenzamine hydrochloride 通常具有更好的水溶性和稳定性。

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Phenoxybenzamine Chemical Structure

Phenoxybenzamine Chemical Structure

CAS No. : 59-96-1

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Phenoxybenzamine 的其他形式现货产品:

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

Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[1][2].

IC50 & Target

α-adrenoceptor[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
15.1 μM
Compound: phenoxybenzamine
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
体外研究
(In Vitro)

Phenoxybenzamine hydrochloride (0-100 μM; 96 h) markedly inhibits U251 and U87MG cells proliferation[2].
Phenoxybenzamine hydrochloride (10 μM; 24 h or 72 h) inhibits migration and invasion of U251 and U87MG cells[2].
Phenoxybenzamine hydrochloride (10 μM; 12 h) activates LINGO-1 and inhibits the TrkB-Akt pathway[2].
Phenoxybenzamine (0.1 μM-1 mM; 0-16 h) prevents hippocampal cell death after oxygen glucose deprivation[3].

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

Cell Proliferation Assay[2]

Cell Line: U251 and U87MG cells
Concentration: 0.1, 1, 10, 50 and 100 μM
Incubation Time: 96 h
Result: Cell proliferation was inhibited markedly, the inhibition rate being 26.5 % for U251 cells and 27.3 % for U87MG cells at 10 μM.

Cell Migration Assay [2]

Cell Line: U251 and U87MG cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Apparent inhibition on migration was observed, and the inhibition rate was 28.6 and 39.8 % for U251 and U87MG, respectively.

Cell Invasion Assay[2]

Cell Line: U251 and U87MG cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Attenuated the invasion properties of both U251 and U87MG markedly, as represented by the number of invaded cells per field declining from 365/field to 132/field (36.2 %) for U251 and 444/field to 298/field (67.1 %) for U87MG.

Western Blot Analysis[2]

Cell Line: U251
Concentration: 10 μM
Incubation Time: 12 h
Result: Decreased the protein level of TrkB, p-TrkB, and p-Akt, but Akt remained unchanged significantly.
体内研究
(In Vivo)

Phenoxybenzamine hydrochloride (20 nM; s.c.; 2-day interval for 26 days) shows anti-tumorigenic effect in mice[2].
Phenoxybenzamine (1.0 mg/kg; i.v.; daily for 30 days) is neuroprotective in a rat model of severe traumatic brain injury[3].

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

Animal Model: Nude mice, U87MG tumor model[2]
Dosage: 20 nM
Administration: Subcutaneous injection, 2-day interval for 26 days
Result: Reduced the tumor cells.
Animal Model: Male Wistar rats (350–500 g), traumatic brain injury (TBI) model[3]
Dosage: 1.0 mg/kg
Administration: Intravenous injection, daily for 30 days
Result: Showed significant improvements in neurological severity score (NSS) and foot fault scoring on days 14, 21, and 30. Reduced cognitive impairment associated with severe TBI and reduced the expression of pro-inflammatory genes.
Clinical Trial
分子量

303.83

Formula

C18H22ClNO

CAS 号
中文名称

酚苄明

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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