Tolperisone hydrochloride

Name: Tolperisone hydrochloride
Brand: MedChemExpress
SKU: HY-B1139
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1139 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Tolperisone hydrochloride Chemical Structure

CAS No. : 3644-61-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 32	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tolperisone hydrochloride:

Tolperisone-d₁₀ hydrochloride Get quote

1 Publications Citing Use of MCE Tolperisone hydrochloride

•Front Pharmacol. 2019 Sep 12;10:993. [Abstract]

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

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.

Cell Cycle Analysis^[1]

Cell Line:	AGS, A375, 8505C, and RKO cells
Concentration:	100 μM
Incubation Time:	48 h
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.

Western Blot Analysis^[1]

Cell Line:	AGS, A375, 8505C, and RKO cells
Concentration:	0-150 μM
Incubation Time:	12 h
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.

In Vivo

Tolperisone (25-100 mg/kg) shows antinociceptive effect in partial sciatic nerve ligation (pSNL) evoked neuropathic pain rats^[2].
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.

Animal Model:	rats with partial sciatic nerve ligation (pSNL) evoked neuropathic pain^[2]
Dosage:	25-100 mg/kg
Administration:	p.o.
Result:	Restored the developed mechanical allodynia 60, 120, and 180 min after treatment. Reduced elevated Cerebrospinal Fluid (CSF) glutamate level.

Clinical Trial

Molecular Weight

281.82

Formula

C₁₆H₂₄ClNO

CAS No.

3644-61-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C)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:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5484 mL	17.7418 mL	35.4836 mL
5 mM	0.7097 mL	3.5484 mL	7.0967 mL
10 mM	0.3548 mL	1.7742 mL	3.5484 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: ≥ 2.5 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 25 mg/mL (88.71 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.94%

Select Batch:

Data Sheet (288 KB) SDS (393 KB)

COA (245 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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

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.