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

Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD).

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

Guanfacine hydrochloride Chemical Structure

Guanfacine hydrochloride Chemical Structure

CAS No. : 29110-48-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 38 In-stock
10 mg USD 60 In-stock
50 mg USD 192 In-stock
100 mg USD 295 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Guanfacine hydrochloride:

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Guanfacine hydrochloride

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)[1][2][3].

IC50 & Target

α adrenergic receptor

 

In Vitro

Guanfacine (hydrochloride) increases the delay-related neuronal firing needed for working memory on dIPFC neurons at the cellular level[1][2].
Guanfacine improves PFC cognitive function by inhibiting the production of CAMP, closing HCN channels, and strengthening the PFC networks[1][2].

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

In Vivo

Guanfacine (hydrochloride) enhances PFC working memory function in aged monkeys and improves impulse control in monkeys performing a delayed discounting task[1][2].
Guanfacine improves cognitive performance when infused directly into the rat or monkey PFC[1][2].
Guanfacine blocks 2A receptors in the monkey dIPFC markedly impairs working memory, behavioral inhibition and greatly reduces persistent neuronal firing[1][2].

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

Clinical Trial
Molecular Weight

282.55

Formula

C9H10Cl3N3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC(N)=N)CC1=C(Cl)C=CC=C1Cl.[H]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 : ≥ 30 mg/mL (106.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (70.78 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5392 mL 17.6960 mL 35.3920 mL
5 mM 0.7078 mL 3.5392 mL 7.0784 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
=
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 (8.85 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 (8.85 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.
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 3.5392 mL 17.6960 mL 35.3920 mL 88.4799 mL
5 mM 0.7078 mL 3.5392 mL 7.0784 mL 17.6960 mL
10 mM 0.3539 mL 1.7696 mL 3.5392 mL 8.8480 mL
15 mM 0.2359 mL 1.1797 mL 2.3595 mL 5.8987 mL
20 mM 0.1770 mL 0.8848 mL 1.7696 mL 4.4240 mL
25 mM 0.1416 mL 0.7078 mL 1.4157 mL 3.5392 mL
30 mM 0.1180 mL 0.5899 mL 1.1797 mL 2.9493 mL
40 mM 0.0885 mL 0.4424 mL 0.8848 mL 2.2120 mL
50 mM 0.0708 mL 0.3539 mL 0.7078 mL 1.7696 mL
60 mM 0.0590 mL 0.2949 mL 0.5899 mL 1.4747 mL
DMSO 80 mM 0.0442 mL 0.2212 mL 0.4424 mL 1.1060 mL
100 mM 0.0354 mL 0.1770 mL 0.3539 mL 0.8848 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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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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Guanfacine hydrochloride
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