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Phenoxybenzamine hydrochloride

Catalog No. T1158 CAS 63-92-3

Synonyms: NCI-c01661, NSC 37448, Phenoxybenzamine HCl

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

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Phenoxybenzamine hydrochloride Chemical Structure

Phenoxybenzamine hydrochloride, CAS 63-92-3

Pack Size	Availability	Price/USD	Quantity
1 g	In stock	$ 42.00
1 mL * 10 mM (in DMSO)	In stock	$ 30.00

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Purity: 100%

Purity: 98.04%

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Description	Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.
In vitro	The IC50 (100 nM) derived from the blockade of [3H]yohimbine binding by Phenoxybenzamine hydrochloride is significantly less than the IC50 (550 nM) for the corresponding reversal by Phenoxybenzamine hydrochloride of the effects of norepinephrine on cyclic AMP accumulation[1]. 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). In addition, combined treatment with Phenoxybenzamine hydrochloridetolamine and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride combined treatment. Combined treatment with high concentrations of dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with combined treatment with low concentrations of dexmedetomidine (300 nM) and Phenoxybenzamine hydrochloride[2].
In vivo	Phenoxybenzamine hydrochloride (20 nM, s.c.) effectively suppresses the tumorigenesis of glioma cells in mice and the cell density in Phenoxybenzamine hydrochloride-U87 mg xenografts decreases significantly[3]. Phenoxybenzamine hydrochloride (1 mg/kg, i.v.) treated rats shows significant improvements in NSS and foot fault scoring[4].
Cell Research	Phenoxybenzamine hydrochloride is dissolved in DMSO. After cytometry, 1×3 cells are implanted in a 96-well plate in 100 μL DMEM supplemented with 10 % FBS. Ten microliter (10 % of the total volume) WST-1 (Water Soluble Tetrazolium) is added to cells and incubated at 37°C for 30 min before colorimetric assay with 450 nm excitation and 630 nm emission at 24 h intervals up to 96 h. The mean fluorescence value is counted, and the cell number is determined using the standard curve.

Synonyms	NCI-c01661, NSC 37448, Phenoxybenzamine HCl
Molecular Weight	340.3
Formula	C18H23Cl2NO
CAS No.	63-92-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 63 mg/mL (185.1 mM)

H2O: 14 mg/mL (41.1 mM)

DMSO: 63 mg/mL (185.1 mM)

References and Literature

1. Lenox, R.H., et al, Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve. Mol Pharmacol, 1985. 27(1): p. 1-9. 2. Byon HJ, 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. 3. Lin XB, et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016 Mar;37(3):2901-8. 4. 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.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Inhibitor Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Drug Library GPCR Compound Library

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Keywords

Phenoxybenzamine hydrochloride 63-92-3 GPCR/G Protein Neuroscience Adrenergic Receptor CaMK pheochromocytoma Beta Receptor NCI-c01661 neuroprotective Phenoxybenzamine Hydrochloride NSC 37448 Inhibitor Phenoxybenzamine antitumor NSC37448 hypertension NSC-37448 inhibit Phenoxybenzamine HCl glioma inhibitor

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