1. Metabolic Enzyme/Protease Apoptosis
  2. Carbonic Anhydrase Apoptosis
  3. Zonisamide

Zonisamide  (Synonyms: AD 810; CI 912)

Cat. No.: HY-B0124 Purity: 99.85%
COA Handling Instructions

Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy.

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

Zonisamide Chemical Structure

Zonisamide Chemical Structure

CAS No. : 68291-97-4

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Based on 1 publication(s) in Google Scholar

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Description

Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy[1][2][3][4].

IC50 & Target

CA Ⅱ

 

In Vitro

Zonisamide (10, 50, 100, 200 μM; 24 h) increases viability of SH-SY5Y cells via an anti-apoptotic effect[1].
Zonisamide (100 μM; 24 h) shows neuroprotective effects in PD-cellular models. (PD: parkinson’s disease)[1].
Zonisamide (100 μM; 24 h) reduces levels of proapoptotic molecules, and upregulates levels of MnSOD (MnSOD over-expression attenuates MPTP toxicity and protects cells from apoptosis)[1].
Zonisamide (0.1, 0.3, 1 μM; 24 h) inhibits cardiac hypertrophy and fibrosis in vitro[3].
Zonisamide markedly increases the expression of Hrd1 in Ang II-treated NRCMs[3].

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

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 10, 50, 100, 200 µM
Incubation Time: 24 h
Result: Induced an increase of cell viability, and with the greatest effect being at 100 µM.
Exhibited neuroprotective effect on SH-SY5Y cells (PD-cellular models) when at 100 µM.

Apoptosis Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 100 µM
Incubation Time: 24 h
Result: Showed an effect of anti-apoptotic.

RT-PCR[3]

Cell Line: NRCMs and cardiac fibroblasts (expose to Ang II for cardiomyocyte hypertrophy and fibrosis model)
Concentration: 0.1, 0.3, 1 μM
Incubation Time: 24 h
Result: Decreased the expression of atrial natriuretic factor (ANF) and cardiomyosin heavy chain β (β-MHC) but increased the expression of cardiac myosin heavy chain α (α-MHC) in NRCMs.
Decreased cardiac expression of the fibrosis-related gene Collagen 1A1 (Col1A1) in cardiac fibroblasts.

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 100 µM
Incubation Time: 24 h
Result: Reduced the proapoptotic molecules levels of cleaved caspase-9, -3, and p-JNK, and blocked the activation of proapoptotic molecules in SH-SY5Y cells. Induced an increase in MnSOD levels.(MnSOD over-expression attenuates MPTP toxicity and protects cells from apoptosis).
In Vivo

Zonisamide (40 mg/kg; i.p.; single daily for 14 days) prevents seizures in FeCl3-induced chronic amygdalar seizures model[2].
Zonisamide (14, 28, 56 mg/kg; i.p.; single daily for 6 weeks) alleviates cardiac hypertrophy and improved cardiac function in rats subjected to AAC (abdominal aortic constriction)[3].
Zonisamide (14, 28, 56 mg/kg; i.p.; single daily for 6 weeks) upregulates Hrd1 expression and accelerates ERAD in the hearts of AAC rats[3].

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

Animal Model: Male Wistar rats (200-250 g; FeCl3-induced chronic amygdalar seizures)[2].
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; single daily for 14 days.
Result: Showed activity of anti-seizures.
Significantly down-regulated GABA transporters GAT-1 in the hippocampus.
Animal Model: Adult male Sprague-Dawley rats (100-120 g; cardiac hypertrophy model)[3].
Dosage: 14, 28, 56 mg/kg
Administration: Intraperitoneal injection; single daily for 6 weeks.
Result: Significantly attenuated cardiac hypertrophy and fibrosis.
Increased LV ejection fraction (EF), fractional shortening (FS) and E/A ratio.
Markedly increased the expression of Hrd1 in the hearts of AAC rats.
Clinical Trial
Molecular Weight

212.23

Formula

C8H8N2O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(CC1=NOC2=C1C=CC=C2)(N)=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: 

DMSO : 250 mg/mL (1177.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.67 mg/mL (3.16 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7119 mL 23.5593 mL 47.1187 mL
5 mM 0.9424 mL 4.7119 mL 9.4237 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (9.80 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 (9.80 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: 1 mg/mL (4.71 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • Protocol 2

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 25 mg/mL (117.80 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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.85%

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 4.7119 mL 23.5593 mL 47.1187 mL 117.7967 mL
DMSO 5 mM 0.9424 mL 4.7119 mL 9.4237 mL 23.5593 mL
10 mM 0.4712 mL 2.3559 mL 4.7119 mL 11.7797 mL
15 mM 0.3141 mL 1.5706 mL 3.1412 mL 7.8531 mL
20 mM 0.2356 mL 1.1780 mL 2.3559 mL 5.8898 mL
25 mM 0.1885 mL 0.9424 mL 1.8847 mL 4.7119 mL
30 mM 0.1571 mL 0.7853 mL 1.5706 mL 3.9266 mL
40 mM 0.1178 mL 0.5890 mL 1.1780 mL 2.9449 mL
50 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.3559 mL
60 mM 0.0785 mL 0.3927 mL 0.7853 mL 1.9633 mL
80 mM 0.0589 mL 0.2945 mL 0.5890 mL 1.4725 mL
100 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1780 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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Zonisamide
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