2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. Ethosuximide

Ethosuximide, a widely prescribed anti-epileptic agent, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.

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Ethosuximide Chemical Structure

Ethosuximide Chemical Structure

CAS No. : 77-67-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Ethosuximide:

Ethosuximide Related Antibodies

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Description

Ethosuximide, a widely prescribed anti-epileptic agent, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.

IC50 & Target

T-type calcium channel

 

In Vitro

The efficacy of Ethosuximide in generalized absence epilepsy is thought to be due to blockade of the low voltage activated T-type calcium channel. There is no reduction in total Tau levels in Ethosuximide treated Tau transgenic worms as compare to vehicle controls. The rescuing effect of Ethosuximide is therefore not due to transgene suppression or reduced expression of toxic mutant Tau protein. Quantification of the amount of soluble and insoluble (RIPA-extractable) Tau relative to total Tau levels reveals a significant reduction in aberrantly-folded, insoluble Tau and a corresponding increase in soluble Tau in Ethosuximide-treated compare with untreated worms[1]. Concentrations of 2 μM or more of Ethosuximide not only are found to be less effective than 1 μM concentration of Ethosuximide, but also induce cell toxicity. GABA staining immuno uorescence images show that after treatment with Ethosuximide, GABA positive neuron increases by 3 and 6.5 fold for concentrations of 0.1 and 1 μM, respectively. BrdU staining shows nuclei proliferation after 2 to 3 days of Ethosuximide exposure. The mean of nuclei is 15.98±0.41 for the low concentration of Ethosuximide while it is 25.27±0.48 for the high concentration after Brdu staining. This number is 11.05±0.2 for lithium chloride[2].

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

Ethosuximide Related Antibodies
Clinical Trial
Molecular Weight

141.17

Formula

C7H11NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C)(CC)C1)NC1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (708.37 mM; Need ultrasonic)

DMSO : 100 mg/mL (708.37 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 7.0837 mL 35.4183 mL 70.8366 mL
5 mM 1.4167 mL 7.0837 mL 14.1673 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (14.73 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 (14.73 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.
In Vivo Dissolution Calculator
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.
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: 99.26%

COA (252 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Vehicle- and Ethosuximide-treated Tau V337M worms are lysed and separated into soluble and insoluble fractions. Fractions are separated by SDS-PAGE and western blotted using anti-human Tau T46 and anti-actin antibodies. The abundance of Tau protein in each fraction is quantified by densitometry and normalized against beta-actin. Total Tau levels in lysates are expressed as the percentage of actin-normalized Tau relative to vehicle control lysates; Tau levels in sequentially extracted fractions are expressed as the percentage of actin-normalized Tau relative to the sum of both fractions (soluble+RIPA) combined[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay

Neuronal stem cells from the forebrain Cortex of a 3-day-old rat are used in this study. The cells are differentiated by withdrawal of basic fibroblastic growth factor (bFGF) and exposed to Ethosuximide at two concentrations of 0.1 μM and 1 μM. Before drug treatment, the cells are rinsed once with PBS, and the medium is replaced with fresh, bFGF-free DMEM/F12 medium containing different concentration of Ethosuximide. Medium exchange is done every day for 6 days with medium containing Ethosuximide. Then, cells are fixed for immunocytochemistry[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 7.0837 mL 35.4183 mL 70.8366 mL 177.0915 mL
5 mM 1.4167 mL 7.0837 mL 14.1673 mL 35.4183 mL
10 mM 0.7084 mL 3.5418 mL 7.0837 mL 17.7091 mL
15 mM 0.4722 mL 2.3612 mL 4.7224 mL 11.8061 mL
20 mM 0.3542 mL 1.7709 mL 3.5418 mL 8.8546 mL
25 mM 0.2833 mL 1.4167 mL 2.8335 mL 7.0837 mL
30 mM 0.2361 mL 1.1806 mL 2.3612 mL 5.9030 mL
40 mM 0.1771 mL 0.8855 mL 1.7709 mL 4.4273 mL
50 mM 0.1417 mL 0.7084 mL 1.4167 mL 3.5418 mL
60 mM 0.1181 mL 0.5903 mL 1.1806 mL 2.9515 mL
80 mM 0.0885 mL 0.4427 mL 0.8855 mL 2.2136 mL
100 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7709 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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Ethosuximide 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.

Keywords:

Ethosuximide77-67-8Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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