1. Membrane Transporter/Ion Channel Neuronal Signaling Apoptosis
  2. nAChR Apoptosis
  3. Hexamethonium Bromide

Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models.

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Hexamethonium Bromide Chemical Structure

Hexamethonium Bromide Chemical Structure

CAS No. : 55-97-0

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Based on 3 publication(s) in Google Scholar

Other Forms of Hexamethonium Bromide:

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Description

Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models[1][2][3][4].

IC50 & Target

nAChR[1]

In Vitro

Hexamethonium Bromide (100 μM; 60 minutes) abolishes epibatidine-induced depolarisations of smooth muscle cells[1].
The α3β4α5 receptors have greater sensitivity to Hexamethonium Bromide than the other potential ganglionic models, α3β4, α3β2, and α3β2α5[2].

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

In Vivo

Hexamethonium Bromide (0.2-25 mg/kg; i.v.) significantly reduces the renal sympathetic nerve activity (RSNA), mean arterial pressure (MAP) and heart rate (HR) in the Wistar rats and the spontaneously hypertensive rats (SHRs)[4].
Hexamethonium Bromide (0.2-1.0 mg/kg; i.v.) treatments show no significant differences in the RSNA, MAP or HR between Wistar rats and SHRs[4].
Hexamethonium Bromide (5.0-25 mg/kg; i.v.) results in a greater reduction in the RSNA and MAP in SHRs compared with Wistar rats[4].

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

Animal Model: Male normotensive Wistar rats (280-320 g), SHRs[4]
Dosage: 0.2 mg/kg, 1.0 mg/kg, 5.0 mg/kg, 25 mg/kg
Administration: Intravenous injection
Result: Significantly reduced the RSNA, MAP and HR in the Wistar rats and the SHRs.
Molecular Weight

362.19

Formula

C12H30Br2N2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[N+](C)(C)CCCCCC[N+](C)(C)C.[Br-].[Br-]

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: 

H2O : ≥ 100 mg/mL (276.10 mM)

DMSO : 16.67 mg/mL (46.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7610 mL 13.8049 mL 27.6098 mL
5 mM 0.5522 mL 2.7610 mL 5.5220 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.67 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (276.10 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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 / H2O 1 mM 2.7610 mL 13.8049 mL 27.6098 mL 69.0245 mL
5 mM 0.5522 mL 2.7610 mL 5.5220 mL 13.8049 mL
10 mM 0.2761 mL 1.3805 mL 2.7610 mL 6.9025 mL
15 mM 0.1841 mL 0.9203 mL 1.8407 mL 4.6016 mL
20 mM 0.1380 mL 0.6902 mL 1.3805 mL 3.4512 mL
25 mM 0.1104 mL 0.5522 mL 1.1044 mL 2.7610 mL
30 mM 0.0920 mL 0.4602 mL 0.9203 mL 2.3008 mL
40 mM 0.0690 mL 0.3451 mL 0.6902 mL 1.7256 mL
H2O 50 mM 0.0552 mL 0.2761 mL 0.5522 mL 1.3805 mL
60 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1504 mL
80 mM 0.0345 mL 0.1726 mL 0.3451 mL 0.8628 mL
100 mM 0.0276 mL 0.1380 mL 0.2761 mL 0.6902 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Hexamethonium Bromide
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HY-B0569
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