1. Anti-infection Neuronal Signaling GPCR/G Protein
  2. Parasite Adrenergic Receptor
  3. Guanabenz hydrochloride

Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure.

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Guanabenz hydrochloride Chemical Structure

Guanabenz hydrochloride Chemical Structure

CAS No. : 23113-43-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Guanabenz hydrochloride:

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Description

Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure[1][2][3].

IC50 & Target

Toxoplasma

 

In Vitro

Guanabenz hydrochloride (0.5-50 μM, 24 h) is treated with increasing concentrations for 24 hours not affect cell viability[1].
Guanabenz hydrochloride (0.5-50 μM, 24 h) alone not affects the UPR targets, neither on mRNA or protein level nor the phosphorylation status of eIF2a. Guanabenz also not induces GADD34 or the constitutively active form CReP[1].
Guanabenz hydrochloride (0.5-50 μM, 24 h) alone not induces ER stress in neonatal rat cardiomyocytes[1].

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

Cell Viability Assay[1]

Cell Line: Neonatal rat cardiac myocytes (NRCM)
Concentration: 0.5-50 μM
Incubation Time: 24 h
Result: Did not affect cell survival.

Western Blot Analysis[1]

Cell Line: Neonatal rat cardiac myocytes (NRCM)
Concentration: 0.5-50 μM
Incubation Time: 24 h
Result: Increased the levels of low panel concentration-dependent UPR targets proteins.

RT-PCR[1]

Cell Line: Neonatal rat cardiac myocytes (NRCM)
Concentration: 0.5-50 μM
Incubation Time: 24 h
Result: Did not affect levels of UPR targets.
In Vivo

Guanabenz hydrochloride (5 mg/kg/day; i.p.; for 3 weeks) can reproducibly reduce brain cyst burden[2].
Guanabenz hydrochloride (5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice[2].
Guanabenz hydrochloride (100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min) reduces sympathetic outflow, heart rate and blood pressure in debuffered cats[3].

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

Animal Model: BALB/cJ mice[2]
Dosage: 5 mg/kg
Administration: 5 mg/kg/day; i.p. ; for 3 weeks
Result: Reduced the latent brain cysts in both male and female BALB/cJ mice.
Animal Model: BALB/cJ mice[2]
Dosage: 5 mg/kg; 10 mg/kg
Administration: 5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks
Result: Reversed parasite-induced hyperactivity to near-baseline levels.
Animal Model: Cats[3]
Dosage: 100 and 320 μg/kg and 1 mg/kg
Administration: 100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min
Result: Declined markedly blood pressure and nerve activity.
Clinical Trial
Molecular Weight

267.54

Formula

C8H9Cl3N4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(/C=N/NC(N)=N)C(Cl)=CC=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (373.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7378 mL 18.6888 mL 37.3776 mL
5 mM 0.7476 mL 3.7378 mL 7.4755 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 and light). 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 (9.34 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 (9.34 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 and light)

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 and light). 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 3.7378 mL 18.6888 mL 37.3776 mL 93.4440 mL
5 mM 0.7476 mL 3.7378 mL 7.4755 mL 18.6888 mL
10 mM 0.3738 mL 1.8689 mL 3.7378 mL 9.3444 mL
15 mM 0.2492 mL 1.2459 mL 2.4918 mL 6.2296 mL
20 mM 0.1869 mL 0.9344 mL 1.8689 mL 4.6722 mL
25 mM 0.1495 mL 0.7476 mL 1.4951 mL 3.7378 mL
30 mM 0.1246 mL 0.6230 mL 1.2459 mL 3.1148 mL
40 mM 0.0934 mL 0.4672 mL 0.9344 mL 2.3361 mL
50 mM 0.0748 mL 0.3738 mL 0.7476 mL 1.8689 mL
60 mM 0.0623 mL 0.3115 mL 0.6230 mL 1.5574 mL
80 mM 0.0467 mL 0.2336 mL 0.4672 mL 1.1680 mL
100 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.9344 mL
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Guanabenz 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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Guanabenz hydrochloride
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