Cat. No.: HY-B0194A

Tizanidine hydrochloride

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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).

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

Purity: 99.93%
CAS No.: 64461-82-1
Formula: C₉H₉Cl₂N₅S
Molecular Weight:290.17

Storage:

4°C, sealed storage, away from moisture

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

Tizanidine hydrochloride Chemical Structure

CAS No.: 64461-82-1

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

α adrenergic receptor

All Adrenergic Receptor Isoforms :

All Akt Isoforms :

All Wnt Isoforms :

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.

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.

Chemical Information

CAS No. 64461-82-1
Appearance Solid
Molecular Weight 290.17
Formula C₉H₉Cl₂N₅S
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4463 mL

17.2313 mL

34.4626 mL

5 mM

0.6893 mL

3.4463 mL

6.8925 mL

10 mM

0.3446 mL

1.7231 mL

3.4463 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kamen L, et al. A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury. Curr Med Res Opin. 2008 Feb;24(2):425-39. [Content Brief]

[2]. Granfors MT, Backman JT, Laitila J, Neuvonen PJ. Tizanidine is mainly metabolized by cytochrome p450 1A2 in vitro. Br J Clin Pharmacol. 2004 Mar;57(3):349-53. doi: 10.1046/j.1365-2125.2003.02028.x. PMID: 14998432; PMCID: PMC1884447. [Content Brief]

[3]. Zhao L, Zhao G, Xue Q. Tizanidine (Hydrochloride) Inhibits A549 Lung Cancer Cell Proliferation and Motility Through Regulating Nischarin. Onco Targets Ther. 2020 Jan 10;13:291-298. [Content Brief]

[4]. Rodríguez-Palma EJ, et al. Sex-dependent antiallodynic effect of α2 adrenergic receptor agonist tizanidine in rats with experimental neuropathic pain. Eur J Pharmacol. 2022 Apr 5;920:174855. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMSO	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

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All Adrenergic Receptor Isoforms

All Akt Isoforms

All Wnt Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table