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Ethosuximide Calcium Channel inhibitor

Name: Ethosuximide
Brand: Selleck Chemicals
SKU: S4626
Availability: InStock
Rating: 5 (1 reviews)

Catalog No.S4626 Purity:99.84%

Ethosuximide(Zarontin) is a succinimide anticonvulsant, used mainly in absence seizures; A calcium channel blocker.

Chemical Structure

Molecular Weight: 141.17

Purity & Quality Control

Batch: Purity: 99.84%

99.84

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Signaling Pathway

Calcium Channel Signaling Pathway

Mechanism of Action

In vitro
In vitro	Ethosuximide(ETH) enhances hippocampal derived NSC proliferation and neurospheres formation in vitro. Low concentration of ETH induces proliferation of NSC, while higher concentrations of ETH are cytotoxic. Also, ETH activates the PI3K/Akt signal transduction pathway in adult hippocampal NSC in vitro. Blockade of the PI3K/Akt pathway inhibits ETH induced hippocampal NSC neuronal differentiation^[3].
Cell Research	Cell lines	Mouse neuroblastoma cell line (N2A)
	Concentrations	0.1, 0.56, 1 mg/ml
	Incubation Time	5 h
	Method	Mouse Neuro2A (N2A) neuroblastoma cells are cultured on 6-well plates and treated with retinoic acid to induce neuronal differentiation. After 24 h, N2A cells are treated with vehicle control (PBS) or increasing concentrations of ethosuximide for 5 h. Total RNA is then isolated, DNase-treated and reverse transcribed to cDNA. qRT-PCR is run above normalising to the reference genes glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and β-actin (ACTB).

In Vivo
In vivo	Anti-epileptic drug ethosuximide rescues the short lifespan and chemosensory defects exhibited by C. elegans null mutants of dnj-14, the worm orthologue of the DNAJC5 gene mutated in autosomal-dominant adult-onset neuronal ceroid lipofuscinosis. It also ameliorates the locomotion impairment and short lifespan of worms expressing a human Tau mutant that causes frontotemporal dementia^[1]. Ethosuximide extends lifespan by inhibiting the function of specific chemosensory neurons^[2]. It increases neurogenesis, reduces neurodegeneration, and reverses cognitive impairments in rat model of AD like phenotypes^[3].
Animal Research	Animal Models	Adult Wistar rats
	Dosages	125 mg/kg
	Administration	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02973542	Unknown status	Irritable Bowel Syndrome	University Hospital Clermont-Ferrand\|SFETD (Socièté Française d''Etude et de Traitement de la Douleur)	April 30 2018	Phase 2
NCT02100046	Completed	Neuropathic Traumatic Pain\|Pain NRS ≥ 4\|Peripheral Neuropathic Pain\|Neuropathic Pain Diagnostic Questionnaire (DN4) ≥ 4	University Hospital Clermont-Ferrand\|Fondation Apicil	March 2014	Phase 2

References

https://pubmed.ncbi.nlm.nih.gov/26419537/
https://pubmed.ncbi.nlm.nih.gov/18949032/
https://pubmed.ncbi.nlm.nih.gov/26420483/

https://pubmed.ncbi.nlm.nih.gov/2545161/

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Chemical Information

Molecular Weight	141.17	Formula	C₇H₁₁NO₂
CAS No.	77-67-8	SDF	Download SDF
Synonyms	Zarontin
Smiles	CCC1(CC(=O)NC1=O)C

Storage and Stability

Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

DMSO : 28 mg/mL ( (198.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 28 mg/mL

Ethanol : 28 mg/mL

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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