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

Idazoxan hydrochloride  (Synonyms: RX 781094 hydrochloride)

Cat. No.: HY-14561A Purity: 99.32%
COA Handling Instructions

Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.

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

Idazoxan hydrochloride Chemical Structure

Idazoxan hydrochloride Chemical Structure

CAS No. : 79944-56-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 69 In-stock
Solution
10 mM * 1 mL in DMSO USD 69 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 55 In-stock
10 mg USD 88 In-stock
25 mg USD 165 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism[1][2].

IC50 & Target

α adrenergic receptor

 

In Vivo

Idazoxan (0.16-5 mg/kg; subcutaneous injection; for 1 hour; male CD-COBS rats) treatment potently reverses haloperidol-induced catalepsy with an ED50 of 0.25 mg/kg. Idazoxan (0.3 and 2.5 mg/kg) has no effect on extracellular DA and do not modify the rise of extracellular DA induced by haloperidol[1].

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

Animal Model: Male CD-COBS rats injected with 1 mg/kg haloperidol[1]
Dosage: 0.16 mg/kg, 0.31 mg/kg, 0.63 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5.0 mg/kg
Administration: Subcutaneous injection; for 1 hour
Result: Potently reversed haloperidol-induced catalepsy with an ED50 of 0.25 mg/kg.
Clinical Trial
Molecular Weight

240.69

Formula

C11H13ClN2O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.C1(C2OC3=CC=CC=C3OC2)=NCCN1

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 : 125 mg/mL (519.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (415.47 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1547 mL 20.7736 mL 41.5472 mL
5 mM 0.8309 mL 4.1547 mL 8.3094 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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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: ≥ 2.08 mg/mL (8.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 50 mg/mL (207.74 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
H2O / DMSO 1 mM 4.1547 mL 20.7736 mL 41.5472 mL 103.8680 mL
5 mM 0.8309 mL 4.1547 mL 8.3094 mL 20.7736 mL
10 mM 0.4155 mL 2.0774 mL 4.1547 mL 10.3868 mL
15 mM 0.2770 mL 1.3849 mL 2.7698 mL 6.9245 mL
20 mM 0.2077 mL 1.0387 mL 2.0774 mL 5.1934 mL
25 mM 0.1662 mL 0.8309 mL 1.6619 mL 4.1547 mL
30 mM 0.1385 mL 0.6925 mL 1.3849 mL 3.4623 mL
40 mM 0.1039 mL 0.5193 mL 1.0387 mL 2.5967 mL
50 mM 0.0831 mL 0.4155 mL 0.8309 mL 2.0774 mL
60 mM 0.0692 mL 0.3462 mL 0.6925 mL 1.7311 mL
80 mM 0.0519 mL 0.2597 mL 0.5193 mL 1.2984 mL
100 mM 0.0415 mL 0.2077 mL 0.4155 mL 1.0387 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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Idazoxan hydrochloride Related Classifications

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  • 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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Idazoxan hydrochloride
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HY-14561A
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