2. GPCR/G Protein Neuronal Signaling Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt
  3. Adrenergic Receptor Apoptosis Akt Wnt β-catenin
  4. Tizanidine hydrochloride

Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine hydrochloride primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).

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Tizanidine hydrochloride

Tizanidine hydrochloride Chemical Structure

CAS No. : 64461-82-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Tizanidine hydrochloride:

Tizanidine hydrochloride Related Antibodies

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α adrenergic receptor β adrenergic receptor

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Akt Akt1 Akt2 Akt3

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine hydrochloride primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI)[1][2][3][4].

IC50 & Target

α adrenergic receptor

 

In Vitro

Tizanidine hydrochloride is mainly metabolized by cytochrome CYP1A2 and resultes in time- and NADPH-dependent substrate consumption with a half-life of 50 min in human liver microsomes[2].
Tizanidine hydrochloride (20 μM, 0-72 h) inhibits the proliferation, migration and invasion of A549 cells, and induces apoptosis through the regulation of AKT and Wnt3a/β-catenin pathways mediated by Nischarin[3].

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

Tizanidine hydrochloride Related Antibodies

Cell Migration Assay [3]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Decreased the crystal violet-stained cells.

Cell Invasion Assay[3]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Suppressed invasion ability of A549 cells by significant inhibition andmigration ability under the same inhibition.

Apoptosis Analysis[3]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 48 h
Result: Significantly increased the apoptosis rate of A549 cells.

Cell Migration Assay [3]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Decreased Bcl-2 expression, while simultaneous expression of Bax was increased.
Significantly increased the expression of Caspase-3.
Was no change in the expressions of AKT and mTOR, while in the phosphorylated forms p-AKT and p-mTOR decreased.
Decreased expressions of P70 and Cyclin D1.
Led to a significant decrease in the levels of Wnt3a and β-catenin, which suggested that Wnt3a/β-catenin pathway was inactivated.
Down-regulated Nischarin.
In Vivo

Tizanidine (0.02-20 mg/kg, p.o., single dose or for 14 days) hydrochloride demonstrates a stronger analgesic effect in female rats with neuropathic pain and estrogen is identified as the key factor contributing to the gender difference[4].

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

Animal Model: Spinal nerve ligation (SNL) model established in female and male Wistar rats (6-7 weeks, 140-160 g)[4]
Dosage: 0.02, 0.2, 2 and 20 mg/kg
Administration: Oral administration (p.o.), increasing doses for 14 days
Result: Showed dose-dependent analgesic effect, and the magnetic effect is significantly stronger than that in males.
Animal Model: Ovarian removal (OVX) model established in female Wistar rats (6-7 weeks, 140-160 g)[4]
Dosage: 2 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Decreased the TZN AUC in OVX female rats to 90 g·h, which was 50% lower than that of the intact females.
Completed reversal of the OVX effect after E2 replacement therapy.
Clinical Trial
Molecular Weight

290.17

Formula

C9H9Cl2N5S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=C(NC2=NCCN2)C3=NSN=C3C=C1.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 : 50 mg/mL (172.31 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (68.93 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4463 mL 17.2313 mL 34.4626 mL
5 mM 0.6893 mL 3.4463 mL 6.8925 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)

C1

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Volume (start)

V1

=
Concentration (final)

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: ≥ 5 mg/mL (17.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (17.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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

Purity: 99.93%

SDS (393 KB)

COA (254 KB) LCMS (86 KB)

Handling Instructions (2659 KB)
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 3.4463 mL 17.2313 mL 34.4626 mL 86.1564 mL
5 mM 0.6893 mL 3.4463 mL 6.8925 mL 17.2313 mL
10 mM 0.3446 mL 1.7231 mL 3.4463 mL 8.6156 mL
15 mM 0.2298 mL 1.1488 mL 2.2975 mL 5.7438 mL
20 mM 0.1723 mL 0.8616 mL 1.7231 mL 4.3078 mL
25 mM 0.1379 mL 0.6893 mL 1.3785 mL 3.4463 mL
30 mM 0.1149 mL 0.5744 mL 1.1488 mL 2.8719 mL
40 mM 0.0862 mL 0.4308 mL 0.8616 mL 2.1539 mL
50 mM 0.0689 mL 0.3446 mL 0.6893 mL 1.7231 mL
60 mM 0.0574 mL 0.2872 mL 0.5744 mL 1.4359 mL
DMSO 80 mM 0.0431 mL 0.2154 mL 0.4308 mL 1.0770 mL
100 mM 0.0345 mL 0.1723 mL 0.3446 mL 0.8616 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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Tizanidine 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.

Keywords:

Tizanidine64461-82-1Adrenergic ReceptorApoptosisAktWntβ-cateninBeta ReceptorPKBProtein kinase BBeta cateninAdrenergic receptorsAllodyniaNeuropathic painSex-dependentTizanidine hydrochlorideInhibitorinhibitorinhibit

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