Eperisone hydrochloride
Based on 1 Customer Validation
Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.95%
- CAS. Nr.: 56839-43-1
- Formel: C17H26ClNO
- Molecular Weight:295.85
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Speicherung:
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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Chemical Information
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Alle P2X Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Eperisone Hydrochloride (0--200 µM, 18-72 h) preferentially suppresses lung fibroblast activity, but is not toxic to alveolar epithelial cells in vitro[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LL29, HFL-1 and IMR-90 cells
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Concentration:25-200 µM
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Incubation Time:24 h
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Result:Decreased the percentage of viable LL29 cells, HFL-1 and IMR-90 cells in a dose-dependent manner.
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Cell Line:LL29
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Concentration:0-100 μM
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Incubation Time:18 h
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Result:Exhibited cytotoxic effects in a time- and concentration-dependent manner in LL29 cells.
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Cell Line:LL29 cells
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Concentration:10-30 μM
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Incubation Time:72 h
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Result:Suppressed the mRNA expression of Collagen 1a1 (COL1A1), α-SMA (ACTA2), connective tissue growth factor (CTGF), vascular endothelial growth factor (VEGF), basic fibroblast growth factor (BFGF), and platelet-derived growth factor (PDGF-A) increased by TGF-β1 (5 µM, 72 h) in LL29 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BLM-induced pulmonary fibrosis of mice[5]
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Dosage:15 or 50 mg/kg
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Administration:p.o., a single dose for 9 days
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Result:Suppressed the BLM-dependent collagen deposition and the amount of hydroxyproline increased by BLM in a dose-dependent manner.
Decreased the BLM-dependent increase in α-SMA-positive cells and the BLM-dependent increase of Col1a1, Acta2, and Bfgf expression in the lungs of mice.
Chemical Information
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CAS. Nr. 56839-43-1
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Appearance Solid
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Molecular Weight 295.85
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Formel C17H26ClNO
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Color White to off-white
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SMILES
O=C(C1=CC=C(CC)C=C1)C(C)CN2CCCCC2.[H]Cl
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Synonyms
(±)-Eperisone hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
H2O : 100 mg/mL (338.01 mM; Need ultrasonic)
DMSO : 31.25 mg/mL (105.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (7.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 16.67 mg/mL (56.35 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.
Reinheit & Dokumentation
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Data Sheet (276 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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Handling Instructions (2659 KB)
Verweise
[1]. Cabitza P, et al. Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study. Eur Rev Med Pharmacol Sci. 2008 Jul-Aug;12(4):229-35. [Content Brief]
[3]. Bavage S, et al. Clinical efficacy and safety of eperisone for low back pain: A systematic literature review. Pharmacol Rep. 2016 Oct;68(5):903-12. [Content Brief]
[4]. Park KH, Lee SC, Yuk JE, Kim SR, Lee JH, Park JW. Eperisone-Induced Anaphylaxis: Pharmacovigilance Data and Results of Allergy Testing. Allergy Asthma Immunol Res. 2019;11(2):231-240. [Content Brief]
[5]. Tanaka KI, et al. Therapeutic effects of eperisone on pulmonary fibrosis via preferential suppression of fibroblast activity. Cell Death Discov. 2022 Feb 8;8(1):52. [Content Brief]
[6]. Okada M, et al. Eperisone Hydrochloride, a Muscle Relaxant, Is a Potent P2X7 Receptor Antagonist. Chem Pharm Bull (Tokyo). 2024;72(3):345-348. [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 | 3.3801 mL | 16.9005 mL | 33.8009 mL | 84.5023 mL |
| 5 mM | 0.6760 mL | 3.3801 mL | 6.7602 mL | 16.9005 mL | |
| 10 mM | 0.3380 mL | 1.6900 mL | 3.3801 mL | 8.4502 mL | |
| 15 mM | 0.2253 mL | 1.1267 mL | 2.2534 mL | 5.6335 mL | |
| 20 mM | 0.1690 mL | 0.8450 mL | 1.6900 mL | 4.2251 mL | |
| 25 mM | 0.1352 mL | 0.6760 mL | 1.3520 mL | 3.3801 mL | |
| 30 mM | 0.1127 mL | 0.5633 mL | 1.1267 mL | 2.8167 mL | |
| 40 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1126 mL | |
| 50 mM | 0.0676 mL | 0.3380 mL | 0.6760 mL | 1.6900 mL | |
| 60 mM | 0.0563 mL | 0.2817 mL | 0.5633 mL | 1.4084 mL | |
| 80 mM | 0.0423 mL | 0.2113 mL | 0.4225 mL | 1.0563 mL | |
| 100 mM | 0.0338 mL | 0.1690 mL | 0.3380 mL | 0.8450 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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