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Tizanidine
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Catalog No. T7065Cas No. 51322-75-9
Tizanidine, an α2-adrenergic receptor agonist, suppresses the release of neurotransmitters from central nervous system (CNS) noradrenergic neurons.
Tizanidine
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Purity: 99.11%
Catalog No. T7065Cas No. 51322-75-9
Tizanidine, an α2-adrenergic receptor agonist, suppresses the release of neurotransmitters from central nervous system (CNS) noradrenergic neurons.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $30 | In Stock | In Stock | |
| 10 mg | $48 | In Stock | In Stock | |
| 25 mg | $67 | In Stock | In Stock | |
| 50 mg | $88 | In Stock | In Stock | |
| 100 mg | $108 | In Stock | In Stock | |
| 500 mg | $266 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $39 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.11%
Appearance:Solid
Color:Yellow
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Product Introduction
Tizanidine AI Summary
Tizanidine is a biologically active compound with diverse pharmacokinetic and pharmacodynamic properties. It has a partition coefficient (LogD6.5) of -0.68 and a delta logD of -0.81 between pH 6.5 and 7.4. The compound’s ionization constant (pKa) is 8.0, reflecting its ionization behavior. It demonstrates moderate oral bioavailability in humans at 49%, alongside high solubility at pH 7.4 (600 μM) and pH 7.2 (18,250 μg/mL).
In terms of distribution and clearance, Tizanidine has a volume of distribution at steady state (Vdss) of 2.4 L/kg and high binding to plasma proteins with a fraction unbound (Fu) of 0.7. It shows a total body clearance of 11.0 mL/min/kg and a renal clearance of 0.33 mL/min/kg, indicating significant renal excretion and suggesting efficient clearance from the body. The hepatic clearance is low at 10.7 mL/min/kg.
Tizanidine displays bioactivity at several targets. It displaces [125I]PIC from human alpha2 adrenoceptors and human imidazoline receptor 1, with Ki values of 117.9 nM and 28.31 nM respectively, and a selectivity ratio of 0.6197 favoring imidazoline receptor 1. It also inhibits human FAAH at 1 μM concentration, demonstrating 7.43% inhibition. Additionally, it inhibits a range of enzymes and receptors, including moderate inhibition of SARS-CoV-2 3CL-Pro protease and binding activities towards various adrenergic and histamine receptors.
Pharmacodynamically, Tizanidine shows efficacy as an agonist at alpha-2A and alpha-2C adrenergic receptors, inhibiting forskolin-stimulated cAMP accumulation with an EC50 of 86.0 nM for alpha-2A. It presents antiviral activity against SARS-CoV-2 and demonstrated moderate inhibition of induced cytotoxicity in VERO-6 cells at a concentration of 10 μM.
However, Tizanidine is also associated with significant hepatotoxic effects, as evidenced by elevated liver enzymes such as ALT, AST, and others. It can induce conditions like cholelithiasis, cirrhosis, hepatic failure, and hepatitis, suggesting a need for caution in its therapeutic use.
Overall, Tizanidine represents a multi-faceted pharmaceutical agent with notable pharmacological actions and potential bioactivities against various biological targets, but caution is warranted due to its association with liver toxicity..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Tizanidine, an α2-adrenergic receptor agonist, suppresses the release of neurotransmitters from central nervous system (CNS) noradrenergic neurons. |
| Molecular Weight | 253.71 |
| Formula | C9H8ClN5S |
| Cas No. | 51322-75-9 |
| Smiles | N(C=1C=2C(C=CC1Cl)=NSN2)C=3NCCN3 |
| Relative Density. | 1.82 g/cm3 |
| Storage | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.4 mg/mL (17.34 mM), Sonication is recommended.  | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.94 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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