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Eperisone hydrochloride  (Synonyms: (±)-Eperisone hydrochloride)

Cat. No.: HY-B1901 Purity: 99.95%
COA Handling Instructions

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.

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

Eperisone hydrochloride Chemical Structure

Eperisone hydrochloride Chemical Structure

CAS No. : 56839-43-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
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50 mg USD 50 In-stock
100 mg USD 80 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Eperisone hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5][6].

In Vitro

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.

Cell Viability Assay[5]

Cell Line: LL29, HFL-1 and IMR-90 cells
Concentration: 25-200 µM
Incubation Time: 24 h
Result: Decreased the percentage of viable LL29 cells, HFL-1 and IMR-90 cells in a dose-dependent manner.

Cell Cytotoxicity Assay[5]

Cell Line: LL29
Concentration: 0-100 μM
Incubation Time: 18 h
Result: Exhibited cytotoxic effects in a time- and concentration-dependent manner in LL29 cells.

Real Time qPCR[5]

Cell Line: LL29 cells
Concentration: 10-30 μM
Incubation Time: 72 h
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.
In Vivo

Eperisone Hydrochloride (15 or 50 mg/kg, p.o., a single dose for 9 days) suppresses Bleomycin (BLM) (HY-108345)-dependent pulmonary fibrosis through its inhibitory effect on fibroblast activation in the lungs of mice[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BLM-induced pulmonary fibrosis of mice[5]
Dosage: 15 or 50 mg/kg
Administration: p.o., a single dose for 9 days
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.
Clinical Trial
Molecular Weight

295.85

Formula

C17H26ClNO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(CC)C=C1)C(C)CN2CCCCC2.[H]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: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3801 mL 16.9005 mL 33.8009 mL
5 mM 0.6760 mL 3.3801 mL 6.7602 mL
View the 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.

* 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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 16.67 mg/mL (56.35 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: 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

Purity: 99.95%

References

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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Eperisone hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Eperisone hydrochloride
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HY-B1901
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