| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Dihydrokainic acid targets excitatory amino acid transporter 2 (EAAT2/GLT1), the primary glutamate transporter in the central nervous system. It is a selective, non-transportable inhibitor of L-glutamate and L-aspartate uptake. It has a Ki of 23 µM for glutamate uptake by COS cells expressing EAAT2 and is selective for EAAT2 over EAAT1 and EAAT3 (Ki = >3 mM for both).
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| ln Vitro |
In vitro, Dihydrokainic acid inhibits EAAT2-mediated glutamate uptake. By inhibiting EAAT2, it increases extracellular glutamate levels. It has a Ki of 23 µM for glutamate uptake by COS cells expressing EAAT2 and is selective for EAAT2 over EAAT1 and EAAT3 (Ki = >3 mM for both).
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| ln Vivo |
In vivo, Dihydrokainic acid impairs novel object recognition (NOR) memory performance in mice. It has epileptogenic effects. DHK microinfusion (5 nmol) into the rat infralimbic cortex reduces the time spent immobile in the forced swim test, indicating antidepressant-like behavior. DHK microinjection (6.25 nmol) into the rat prefrontal cortex increases the latency to drink sucrose, indicating anhedonia-like behavior.
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| Enzyme Assay |
Dihydrokainic acid's EAAT2 inhibition can be characterized using glutamate uptake assays in COS cells expressing EAAT2. The compound has a Ki of 23 µM for glutamate uptake. Selectivity over EAAT1 and EAAT3 (Ki >3 mM) can also be assessed.
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| Cell Assay |
In vitro cell experiments with Dihydrokainic acid use COS cells expressing EAAT2 to measure glutamate uptake inhibition. Cells are treated with the compound at various concentrations, and glutamate uptake is measured using radiolabeled glutamate or other detection methods. The compound's effects on glutamatergic signaling can be assessed.
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| Animal Protocol |
In vivo animal studies with Dihydrokainic acid involve microinfusion into specific brain regions in rats. Microinfusion (5 nmol) into the infralimbic cortex is used to assess antidepressant-like behavior in the forced swim test. Microinjection (6.25 nmol) into the prefrontal cortex is used to assess anhedonia-like behavior in a sucrose intake test.
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| ADME/Pharmacokinetics |
Dihydrokainic acid has a molecular weight of 215.25 and a molecular formula of C₁₀H₁₇NO₄. The compound is stored as a solid powder at -20°C for long-term storage. It is soluble in DMSO and has a shelf life of >3 years if stored properly.
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| Toxicity/Toxicokinetics |
Dihydrokainic acid is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be stored in a dry, dark place at 0-4°C for short-term storage or -20°C for long-term storage.
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| References |
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| Additional Infomation |
Dihydrokainic acid is a dicarboxylic acid. It is functionally related to ruginic acid.
See also: Dihydroalginate (note moved to). Dihydrokainic acid (DHK) is a glutamate transporter GLT1 (EAAT2) inhibitor. It impairs novel object recognition (NOR) memory performance in mice. It has epileptogenic effects. The compound has a CAS number of 52497-36-6 and is used in research studying glutamatergic signaling and synaptic transmission. |
| Molecular Formula |
C10H17NO4
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|---|---|
| Molecular Weight |
215.24628
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| Exact Mass |
215.116
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| CAS # |
52497-36-6
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| PubChem CID |
107883
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| Appearance |
White to off-white solid powder
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| Density |
1.187g/cm3
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| Boiling Point |
416.6ºC at 760mmHg
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| Melting Point |
285 °C (dec.)
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| Index of Refraction |
1.492
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| LogP |
0.734
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
264
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC(C)[C@H]1CN[C@@H]([C@H]1CC(=O)O)C(=O)O
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| InChi Key |
JQPDCKOQOOQUSC-OOZYFLPDSA-N
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| InChi Code |
InChI=1S/C10H17NO4/c1-5(2)7-4-11-9(10(14)15)6(7)3-8(12)13/h5-7,9,11H,3-4H2,1-2H3,(H,12,13)(H,14,15)/t6-,7+,9-/m0/s1
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| Chemical Name |
(2S,3S,4R)-3-(carboxymethyl)-4-propan-2-ylpyrrolidine-2-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6458 mL | 23.2288 mL | 46.4576 mL | |
| 5 mM | 0.9292 mL | 4.6458 mL | 9.2915 mL | |
| 10 mM | 0.4646 mL | 2.3229 mL | 4.6458 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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