1. Membrane Transporter/Ion Channel
  2. EAAT
  3. Dihydrokainic acid

Dihydrokainic acid is a glutamate transporters (especially GLT1) inhibitor. Dihydrokainic acid targets GLT1 with high affinity, effectively inhibiting its transport function. Dihydrokainic acid exerts its effect by inhibiting the uptake of glutamate, leading to an increase in extracellular glutamate concentration, thereby affecting neuronal excitability and neurotransmission. Dihydrokainic acid is mainly applied in the field of neuroscience for research on glutamate-related neural functions, epilepsy, learning, and memory.

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

Dihydrokainic acid Chemical Structure

Dihydrokainic acid Chemical Structure

CAS No. : 52497-36-6

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Based on 1 publication(s) in Google Scholar

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Description

Dihydrokainic acid is a glutamate transporters (especially GLT1) inhibitor. Dihydrokainic acid targets GLT1 with high affinity, effectively inhibiting its transport function. Dihydrokainic acid exerts its effect by inhibiting the uptake of glutamate, leading to an increase in extracellular glutamate concentration, thereby affecting neuronal excitability and neurotransmission. Dihydrokainic acid is mainly applied in the field of neuroscience for research on glutamate-related neural functions, epilepsy, learning, and memory[1][2][3][4][5].

IC50 & Target

EAAT2

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 3000 μM
Compound: DHK, dihydrokainic acid
Inhibition of glutamate-induced depolarization in human EAAT1 expressed in HEK293 cells by FMP assay
Inhibition of glutamate-induced depolarization in human EAAT1 expressed in HEK293 cells by FMP assay
[PMID: 18578477]
HEK293 IC50
> 3000 μM
Compound: DHK, dihydrokainic acid
Inhibition of glutamate-induced depolarization in human EAAT3 expressed in HEK293 cells by FMP assay
Inhibition of glutamate-induced depolarization in human EAAT3 expressed in HEK293 cells by FMP assay
[PMID: 18578477]
HEK293 IC50
89 μM
Compound: DHK, dihydrokainic acid
Inhibition of glutamate-induced depolarization in human EAAT2 expressed in HEK293 cells by FMP assay
Inhibition of glutamate-induced depolarization in human EAAT2 expressed in HEK293 cells by FMP assay
[PMID: 18578477]
In Vitro

Dihydrokainic acid (5 mM; treating cerebellar slices for 15 min) inhibits the uptake of D-[3H]aspartate by cerebellar slices in a concentration-dependent manner[2].

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

In Vivo

Dihydrokainic acid (1-10 mM; perfused through a dialysis probe; for 60 min; single administration) in the rat dentate gyrus model can evoke epileptiform activity, increase the extracellular concentrations of taurine, alanine, phosphoethanolamine, glutamate, and aspartate, increase the amplitude of population spikes and the PS2:PSI ratio[3]. Dihydrokainic acid (12.5-25 nmol; i.c.v; single administration) in the mouse novel object recognition (NOR) memory model impairs short-term NOR memory performance, long-term NOR memory acquisition, consolidation, and retrieval[4]. Dihydrokainic acid (1-5 mM; perfused through a dialytrode; for 15 min; single administration) can significantly increase the extracellular concentrations of glutamate and taurine in the rat hippocampus (dentate gyrus or CA1 region) model and reduces the field excitatory postsynaptic potential but increases the population spike, while in the CA1 region, it decreases the amplitudes of both the excitatory postsynaptic potential and the spike in the dentate gyrus[5].

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

Animal Model: Kunming strain male mice (male, 35-40 g, not specified age) + novel object recognition (NOR) memory model[4]
Dosage: 6.25, 12.5, 25 nmol (0.01 M PBS, pH 7.4)
Administration: Unilaterally injected into the cerebral ventricle, once at 0.5 h before sampling or 0.5 h before testing
Result: Impaired short-term and long-term NOR memory performance, affecting memory acquisition, consolidation, and retrieval.
Molecular Weight

215.25

Formula

C10H17NO4

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

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: 

H2O : 5 mg/mL (23.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6458 mL 23.2289 mL 46.4578 mL
5 mM 0.9292 mL 4.6458 mL 9.2916 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.

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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: ≥99.0%

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 1 mM 4.6458 mL 23.2289 mL 46.4578 mL 116.1446 mL
5 mM 0.9292 mL 4.6458 mL 9.2916 mL 23.2289 mL
10 mM 0.4646 mL 2.3229 mL 4.6458 mL 11.6145 mL
15 mM 0.3097 mL 1.5486 mL 3.0972 mL 7.7430 mL
20 mM 0.2323 mL 1.1614 mL 2.3229 mL 5.8072 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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Dihydrokainic acid Related Classifications

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Dihydrokainic acid
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