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

Phenoxybenzamine hydrochloride 

Cat. No.: HY-B0431A Purity: ≥98.0%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Phenoxybenzamine hydrochloride Chemical Structure

Phenoxybenzamine hydrochloride Chemical Structure

CAS No. : 63-92-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Phenoxybenzamine hydrochloride:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Phenoxybenzamine hydrochloride

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

α-adrenoceptor[1]

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].

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.
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].

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.
Clinical Trial
Molecular Weight

340.29

Formula

C18H23Cl2NO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(COC1=CC=CC=C1)N(CCCl)CC2=CC=CC=C2.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (293.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9387 mL 14.6933 mL 29.3867 mL
5 mM 0.5877 mL 2.9387 mL 5.8773 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9387 mL 14.6933 mL 29.3867 mL 73.4667 mL
5 mM 0.5877 mL 2.9387 mL 5.8773 mL 14.6933 mL
10 mM 0.2939 mL 1.4693 mL 2.9387 mL 7.3467 mL
15 mM 0.1959 mL 0.9796 mL 1.9591 mL 4.8978 mL
20 mM 0.1469 mL 0.7347 mL 1.4693 mL 3.6733 mL
25 mM 0.1175 mL 0.5877 mL 1.1755 mL 2.9387 mL
30 mM 0.0980 mL 0.4898 mL 0.9796 mL 2.4489 mL
40 mM 0.0735 mL 0.3673 mL 0.7347 mL 1.8367 mL
50 mM 0.0588 mL 0.2939 mL 0.5877 mL 1.4693 mL
60 mM 0.0490 mL 0.2449 mL 0.4898 mL 1.2244 mL
80 mM 0.0367 mL 0.1837 mL 0.3673 mL 0.9183 mL
100 mM 0.0294 mL 0.1469 mL 0.2939 mL 0.7347 mL
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Phenoxybenzamine hydrochloride Related Classifications

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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