2. Induced Disease Models Products Membrane Transporter/Ion Channel
  3. Nervous System Disease Models EAAT
  4. Epilepsy Models
  5. Kainic acid

Kainic acid is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid induces seizures.

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Kainic acid Chemical Structure

Kainic acid Chemical Structure

CAS No. : 487-79-6

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Based on 9 publication(s) in Google Scholar

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Description

Kainic acid is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid induces seizures[1][2].

In Vivo

Kainic acid-induced epilepsy model is an effective tool for studying temporal lobe epilepsy (TLE) and can be administered systemically, into the hippocampus, or amygdala, and is reproducible in various animal models. The systemic Kainic acid model closely resembles human TLE. When Kainic acid (5 nM) is injected into the neostriatum, substantia nigra, or cerebellum, over half of the compound disappears from the injection site and brain within 0.5 hours, with radioactivity detected in other brain regions at concentrations below 7 pM/mg tissue[3][4][6].

1. Induction of epilepsy model in mouse[5]
Background
Kainic acid, an analog of L-glutamate and an ionotropic KA receptor agonist, can damage hippocampal pyramidal neurons.
Specific Mmodeling Methods
Mice: C57BL/6J • male • 7 weeks old • 22 g body weight
Administration: 10 μg in 5 μL • i.c.v.
Note
(1) The right lateral brain ventricle is localized with a stereotactic instrument.
(2) After the operation, skin was sutured, and keep the mice under a warming place until they wake up.
(3) 48 hours after lateral ventricle injection, the mice are anaesthetized using Isoflurane and then sequentially intracardially perfused with saline and PFA (4%, 30 mL). Rapidly remove The mouse brain processed for paraffin embedding or frozen sections.
Modeling Indicators
Electroencephalogram (EEG) recording: Had higher local maximal amplitude and reduced spike frequency compared to the control group.
Histology analysis: Showed Triangulated pyknotic nuclei and cytoplasmic shrinkage in the hippocampal neuron, and induced neuronal loss.
Correlated Product(s): /
Opposite Product(s): Sitagliptin (HY-13749)

2. Induction of epilepsy model in rats[6]
Background
Kainic acid can bind to NMDA receptors which are abundant in neurons in the cornu ammonus of the hippocampus, amygdala, and pyriform cortex, and leading to variable levels of neuronal death in these regions.
Specific Mmodeling Methods
Rat: Sprague-Dawley rats • male
Administration: 10 mg/kg • i.p. • a single dose
Note
(1) Seizures occurres approximately 45 min after injection, typically lasted 2-3 hr.
(2) Kainic acid-treated animals may die during an acute period of intoxication, it's suggested to increase the number of animals per group.
(3) 72 hours later, the rats are anesthetized and immediately perfused transcardially with 50 mL 0.9% saline followed by 500 mL 0.1 m neutral phosphate-buffered formaldehyde (4%). And remove the brain and postfixed at 4°C overnight in the same fixative and dehydrated, embedded in paraffin, and cut into serial 6-μm-thick coronal sections at the level of the dorsal hippocampus.
Modeling Indicators
behavioral changes: Exhibited immobility and rigid postures firstly, followed by repetitive head nodding, ‘wet dog shakes’, and subsequent rearing and falling. Eventually, the rats developed generalized tonic–clonic seizures with continuous convulsions, lasting for several hours.
Histology analysis: Resulted in a loss of pyramidal neurons in fields CA1 and CA3 of the hippocampus.
Increaseed the size, arborization, and stainability of GFAP-immunoreactive cells.
Correlated Product(s): /
Opposite Product(s): Melatonin (HY-B0075)

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

Animal Model: 8 weeks, 200-250 g male adult Wistar rats[1]
Dosage: 5 mg/kg
Administration: I.p.; hourly at least 3 h until status epilepticus
Result: Induced seizures in rats.
Molecular Weight

213.23

Formula

C10H15NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C[C@@H]1[C@@H](C(O)=O)NC[C@@H]1C(C)=C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (187.59 mM; ultrasonic and adjust pH to 3 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 10 mg/mL (46.90 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6897 mL 23.4485 mL 46.8971 mL
5 mM 0.9379 mL 4.6897 mL 9.3794 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. 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)

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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: ≥ 5 mg/mL (23.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (23.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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: 99.96%

COA (255 KB) HNMR (250 KB) RP-HPLC (239 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.6897 mL 23.4485 mL 46.8971 mL 117.2426 mL
5 mM 0.9379 mL 4.6897 mL 9.3794 mL 23.4485 mL
10 mM 0.4690 mL 2.3449 mL 4.6897 mL 11.7243 mL
15 mM 0.3126 mL 1.5632 mL 3.1265 mL 7.8162 mL
20 mM 0.2345 mL 1.1724 mL 2.3449 mL 5.8621 mL
25 mM 0.1876 mL 0.9379 mL 1.8759 mL 4.6897 mL
30 mM 0.1563 mL 0.7816 mL 1.5632 mL 3.9081 mL
40 mM 0.1172 mL 0.5862 mL 1.1724 mL 2.9311 mL
DMSO 50 mM 0.0938 mL 0.4690 mL 0.9379 mL 2.3449 mL
60 mM 0.0782 mL 0.3908 mL 0.7816 mL 1.9540 mL
80 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4655 mL
100 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1724 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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  • 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:

Kainic acid487-79-6EAATExcitatory amino acid transporter Glutamate transporter;Inhibitorinhibitorinhibit

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