Phenoxybenzamine

製品番号: HY-B0431: Data Sheet 取扱説明書
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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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Phenoxybenzamine hydrochloride) usually boasts enhanced water solubility and stability.

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Phenoxybenzamine 構造式

CAS 番号 : 59-96-1

容量		在庫状況
MOQ		Minimum order quantity
50 mg		お問い合わせ
100 mg		お問い合わせ
250 mg		お問い合わせ
Other size		お問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

Other 在庫あり Forms of Phenoxybenzamine:

Phenoxybenzamine hydrochloride

Other Forms of Phenoxybenzamine:

Phenoxybenzamine hydrochloride 在庫あり
Phenoxybenzamine-d₅ hydrochloride お問い合わせ
Phenoxybenzamine (benzyl-2,3,4,5,6-d₅) hydrochloride お問い合わせ
Phenoxybenzamine-d₅ お問い合わせ

顧客検証

•Protein Cell. 2019 Mar;10(3):178-195. [Abstract]

Adrenergic Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

α adrenergic receptor β adrenergic receptor

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

α-adrenoceptor^[1]

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]
HEK293	IC₅₀	2.72 μM Compound: Phenoxybenzamine	TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells	[PMID: 12110607]
HEK293	IC₅₀	4.9 μM Compound: Phenoxybenzamine	TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT2-expressing HEK293 cells TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT2-expressing HEK293 cells	[PMID: 12110607]
HEK293	IC₅₀	6.13 μM Compound: Phenoxybenzamine	TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells	[PMID: 12110607]

体外実験

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].

MedChemExpress (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.

体内実験

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].

MedChemExpress (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.

分子量

303.83

分子式

C₁₈H₂₂ClNO

CAS 番号

59-96-1

SMILES

CC(N(CCCl)CC1=CC=CC=C1)COC2=CC=CC=C2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Habbe N, et al. Urapidil in the preoperative treatment of pheochromocytomas: a safe and cost-effective method. World J Surg. 2013 May;37(5):1141-6. [Content Brief]

[2]. Lin XB, et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016 Mar;37(3):2901-8. [Content Brief]

[3]. Rau TF, et al. Phenoxybenzamine is neuroprotective in a rat model of severe traumatic brain injury. Int J Mol Sci. 2014 Jan 20;15(1):1402-17. [Content Brief]