Home Transmembrane Transporters Sodium Channel inhibitor Tolperisone HCl

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Tolperisone HCl Sodium Channel inhibitor

Cat.No.S4200

Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.
Tolperisone HCl Sodium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 281.82

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Quality Control

Batch: S420001 DMSO]56 mg/mL]false]Water]56 mg/mL]false]Ethanol]56 mg/mL]false Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (198.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 56 mg/mL

Ethanol : 56 mg/mL

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 281.82 Formula

C16H23NO.HCl

 Storage (From the date of receipt)
CAS No. 3644-61-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC=C(C=C1)C(=O)C(C)CN2CCCCC2.Cl

Mechanism of Action

Targets/IC50/Ki
Sodium channel
In vitro
Tolperisone reduces sodium and potassium permeability in the node of Ranvier of frogs, blocks calcium currents in snail neurons and inhibits current through heterologously expressed Nav1.6 channels. Tolperisone hydrochloride represents an effective and safe treatment of painful reflex muscle spasm without the typical side effects of centrally active muscle relaxants.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05544656 Active not recruiting
Low Back Pain
Semmelweis University|National Research Develpment and Innovation Fund Hungary|MEDITOP Pharmaceutical LTD Hungary
 December 13 2019 Phase 3
NCT00532532 Terminated
Muscle Spasticity
Avigen
 September 2007 Phase 2

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