Tolperisone hydrochloride
Based on 2 publication(s) in Google Scholar
Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity.
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- Pureté: 99.84%
- CAS No.: 3644-61-9
- Formule: C16H24ClNO
- Masse moléculaire:281.82
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tolperisone hydrochloride
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Activité biologique
Tolperisone (0-128 μM, 48 h) hydrochloride induces UPR-mediated cancer cell death by directly targeting LSD1, with IC50s of 10-40 μM[1].
Tolperisone inhibits LSD1 activity with an IC50 of 31.09 µM[1].
Tolperisone (100 μM, 48 h) induces cancer cell cycle arrest and apoptosis in AGS, A375, 8505C, and RKO cells[1].
Tolperisone (100 μM, 12 h) repolarizes M2 macrophages into M1 phenotype[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AGS, A375, 8505C, and RKO cells
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Concentration:100 μM
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Incubation Time:48 h
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Result:Induced cell cycle arrest in G2/M phase, and reduced the proportion of cells in S phase.
Decreased the protein expression of Cyclin B1 and CDC25C, and increased the level of p21 and p-CDC25C.
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Cell Line:AGS, A375, 8505C, and RKO cells
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Concentration:0-150 μM
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Incubation Time:12 h
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Result:Increased levels of cleaved caspase-3, cleaved PARP-1, and pro-apoptotic BCL-2 family member Bax.
Increased the levels of p-eIF2α, ATF4, CHOP, and GRP78 in AGS and A375 cells.
Tolperisone (60 mg/kg, once a day for 1 week) hydrochloride inhibits tumor growth in A375 cell-derived xenograft mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:rats with partial sciatic nerve ligation (pSNL) evoked neuropathic pain[2]
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Dosage:25-100 mg/kg
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Administration:p.o.
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Result:Restored the developed mechanical allodynia 60, 120, and 180 min after treatment.
Reduced elevated Cerebrospinal Fluid (CSF) glutamate level.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3644-61-9
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Appearance Solid
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Masse moléculaire 281.82
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Formule C16H24ClNO
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Color White to off-white
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SMILES
O=C(C1=CC=C(C)C=C1)C(C)CN2CCCCC2.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Front Pharmacol
Untargeted Safety Pharmacology Screen of Blood-Activating and Stasis-Removing Patent Chinese Herbal Medicines Identified Nonherbal Ingredients as a Cause of Organ Damage in Experimental Models. [Abstract]2019 Sep 12;10:993. PMID: 31607901 -
Chirality
Evaluation of Acetonitrile in Combination With Alcohols as Modifiers in Chiral Supercritical Fluid Chromatography. [Abstract]2026 Mar 5;38(3):e70092. PMID: 41786509
Solvant et solubilité
DMSO : 100 mg/mL (354.84 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 : 100 mg/mL (354.84 mM; Need ultrasonic)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.87 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.87 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (88.71 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Jiang W, et al. Tolperisone induces UPR-mediated tumor inhibition and synergizes with proteasome inhibitor and immunotherapy by targeting LSD1. Expert Opin Ther Targets. 2023 Jul-Dec;27(9):879-895. [Content Brief]
[2]. Lakatos PP, et al. The Acute Antiallodynic Effect of Tolperisone in Rat Neuropathic Pain and Evaluation of Its Mechanism of Action. Int J Mol Sci. 2022 Aug 24;23(17):9564. [Content Brief]
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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.5484 mL | 17.7418 mL | 35.4836 mL | 88.7091 mL |
| 5 mM | 0.7097 mL | 3.5484 mL | 7.0967 mL | 17.7418 mL | |
| 10 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL | 8.8709 mL | |
| 15 mM | 0.2366 mL | 1.1828 mL | 2.3656 mL | 5.9139 mL | |
| 20 mM | 0.1774 mL | 0.8871 mL | 1.7742 mL | 4.4355 mL | |
| 25 mM | 0.1419 mL | 0.7097 mL | 1.4193 mL | 3.5484 mL | |
| 30 mM | 0.1183 mL | 0.5914 mL | 1.1828 mL | 2.9570 mL | |
| 40 mM | 0.0887 mL | 0.4435 mL | 0.8871 mL | 2.2177 mL | |
| 50 mM | 0.0710 mL | 0.3548 mL | 0.7097 mL | 1.7742 mL | |
| 60 mM | 0.0591 mL | 0.2957 mL | 0.5914 mL | 1.4785 mL | |
| 80 mM | 0.0444 mL | 0.2218 mL | 0.4435 mL | 1.1089 mL | |
| 100 mM | 0.0355 mL | 0.1774 mL | 0.3548 mL | 0.8871 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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