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Tizanidine Adrenergic Receptor agonist

Name: Tizanidine
Brand: Selleck Chemicals
SKU: S5537
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5537

Tizanidine is an imidazoline derivative and a centrally acting α2 adrenergic agonist used as a muscle relaxant for therapy of acute muscle spasms and chronic spasticity.

Chemical Structure

Molecular Weight: 253.71

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Quality Control

Batch: S553701 DMSO]50 mg/mL]false]Water]15 mg/mL]false]Ethanol]6 mg/mL]false Purity: 98.4%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

98.4

Related Targets	AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Adrenergic Receptor Inhibitors	Zenidolol (ICI-118551) Hydrochloride Yohimbine HCl L755507 Atipamezole Higenamine hydrochloride Fenoterol hydrobromide Medetomidine HCl Rauwolscine hydrochloride Deoxycorticosterone acetate Detomidine HCl

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (197.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 15 mg/mL

Ethanol : 6 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.5mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.36mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	253.71	Formula	C₉H₈ClN₅S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	51322-75-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN=C(N1)NC2=C(C=CC3=NSN=C32)Cl

Mechanism of Action

Targets/IC₅₀/Ki	α2 adrenergic receptor
In vitro	Like clonidine, it has sedative, anxiolytic, and analgesic properties, but it has a shorter duration of action and less effect on heart rate and blood pressure.
In vivo	Tizanidine is shown to significantly reduce pain and tissue tenderness and to improve the quality of sleep.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4389556/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01844674	Completed	Malignant Melanoma Neoplasms	Hoffmann-La Roche	September 2 2013	Phase 1
NCT01839279	Completed	Spasticity	Acorda Therapeutics	April 2013	Phase 2
NCT01405950	Terminated	Spasticity Due to Cerebral Palsy	Acorda Therapeutics\|Syneos Health	May 2011	Phase 1
NCT01065987	Completed	Healthy	Dr. Reddy''s Laboratories Limited	September 2001	Phase 1

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