| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
7-Chlorokynurenic acid sodium salt targets the glycine site of the N-methyl-D-aspartate (NMDA) receptor. The NMDA receptor is an ionotropic glutamate receptor that plays a critical role in synaptic plasticity, learning, and memory. The glycine site is a modulatory site on the NMDA receptor that must be occupied by glycine or D-serine for receptor activation. By acting as an antagonist at this site, 7-chlorokynurenic acid sodium salt inhibits NMDA receptor function. The compound acts at the strychnine-insensitive glycine binding site with an IC50 value of 0.56 uM. Its water solubility is improved by the sodium salt form.
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| ln Vitro |
7-Chlorokynurenic acid sodium salt demonstrates potent in vitro activity as an NMDA receptor antagonist. The compound acts at the strychnine-insensitive glycine binding site of the NMDA receptor with an IC50 value of 0.56 uM. It is a potent antagonist of the glycine site of the NMDA receptor. The compound's activity is concentration-dependent, with potent inhibition observed at micromolar concentrations. 7-Chlorokynurenic acid sodium salt is used in neuroscience research to study NMDA receptor function, synaptic plasticity, and excitotoxicity. Its water solubility makes it suitable for various in vitro applications. The compound's activity has been characterized in various in vitro systems.
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| ln Vivo |
Pretreated with 7-chlorokynurate sodium salt (10 nM), male Sprague-Dawley rats exhibit a marked delay in the development of the motor (17.7 ± 2.9 stimulations per day) and electroencephalographic (17.7 ± 2.9 stimulations per day) components of the epileptic response [3].
In vivo, 7-chlorokynurenic acid sodium salt has potent antinociceptive actions after neuraxial delivery. As an NMDA receptor antagonist, the compound has potential therapeutic relevance in conditions such as stroke, epilepsy, and neurodegenerative disorders like Alzheimer's and Huntington's diseases. The compound's ability to cross the blood-brain barrier and its water solubility make it suitable for in vivo studies. Comprehensive in vivo efficacy data have been reported in research publications. The compound's antinociceptive effects after neuraxial delivery suggest potential for pain research applications. |
| Enzyme Assay |
In vitro receptor binding assays for 7-chlorokynurenic acid sodium salt involve measuring binding affinity to the glycine site of the NMDA receptor. Membranes from brain tissue or cells expressing NMDA receptors are incubated with a radiolabeled glycine site ligand (e.g., [3H]-MDL-105,519) and varying concentrations of the test compound. Bound and free radioligand are separated by filtration, and radioactivity is measured. Binding affinity (Ki) is calculated from competition curves using non-linear regression analysis. Functional assays can measure inhibition of NMDA receptor-mediated calcium influx or electrophysiological responses. The compound has an IC50 value of 0.56 uM at the strychnine-insensitive glycine binding site. Each concentration is typically tested in duplicate or triplicate.
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| Cell Assay |
In vitro cellular assays for 7-chlorokynurenic acid sodium salt are performed using neuronal cell cultures or cells expressing NMDA receptors. Cells are treated with NMDA and glycine (or D-serine) to activate the receptor, and calcium influx is measured using fluorescent calcium indicators such as Fluo-4 or Fura-2. Varying concentrations of the test compound are added to assess inhibition of NMDA receptor-mediated responses. Alternatively, electrophysiological recordings can be performed using patch-clamp techniques. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. IC50 values for inhibition of NMDA receptor responses are calculated from dose-response curves. The compound's water solubility makes it suitable for cellular assays.
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| Animal Protocol |
In vivo animal studies for 7-chlorokynurenic acid sodium salt are conducted using rodent models of pain, stroke, epilepsy, and neurodegenerative diseases. The compound is administered via intrathecal, intracerebroventricular, intraperitoneal, or intravenous injection. In pain models, antinociceptive effects are assessed using tail-flick, hot plate, or formalin tests. In stroke models, infarct volume and neurological deficits are assessed. In epilepsy models, seizure activity is monitored. Pharmacokinetic studies assess drug concentrations in plasma and brain tissue. Animals are monitored for clinical signs and body weight. Efficacy is expressed as improvement in behavioral or pathological parameters compared to vehicle-treated controls. The compound's water solubility facilitates administration.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 7-chlorokynurenic acid sodium salt have been characterized in preclinical studies. The compound has a molecular formula of C10H5ClNNaO3 and a molecular weight of 245.59 g/mol. Its chemical name is sodium 7-chloro-4-oxo-1,4-dihydroquinoline-2-carboxylate. The compound is highly water soluble (≥43.4 mg/mL in H2O) and also soluble in DMSO (≥4.64 mg/mL). Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in animal models. The compound's water solubility supports its use in various research applications. Its ability to cross the blood-brain barrier is relevant for its central nervous system effects.
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| Toxicity/Toxicokinetics |
7-Chlorokynurenic acid sodium salt is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As an NMDA receptor antagonist, the compound would be expected to have effects on neurotransmission and synaptic plasticity. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been reported in the public domain. The compound is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
7-Chlorokynurenic acid sodium salt is a potent antagonist of the glycine site of the NMDA receptor with an IC50 of 0.56 uM. It has potent antinociceptive actions after neuraxial delivery. The compound has a molecular formula of C10H5ClNNaO3 and a molecular weight of 245.59 g/mol. It is water soluble (≥43.4 mg/mL in H2O). 7-Chlorokynurenic acid sodium salt is used in neuroscience research to study NMDA receptor function, synaptic plasticity, and excitotoxicity. It has potential therapeutic relevance in stroke, epilepsy, and neurodegenerative disorders. The compound has not entered clinical trials and is available for research purposes only.
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| Molecular Formula |
C10H7CLNNAO3
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| Molecular Weight |
247.61025261879
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| Exact Mass |
244.985
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| CAS # |
1263094-00-3
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| Related CAS # |
7-Chlorokynurenic acid;18000-24-3
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| PubChem CID |
52974249
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
345
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=C1Cl)NC(=CC2=O)C(=O)[O-].[Na+]
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| InChi Key |
IFZYIORLNGNLEI-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C10H6ClNO3.Na/c11-5-1-2-6-7(3-5)12-8(10(14)15)4-9(6)13;/h1-4H,(H,12,13)(H,14,15);/q;+1/p-1
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| Chemical Name |
sodium;7-chloro-4-oxo-1H-quinoline-2-carboxylate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ~50 mg/mL (~203.59 mM)
DMSO : ≥ 33.67 mg/mL (~137.10 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.67 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.67 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.67 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 6.67 mg/mL (27.16 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0386 mL | 20.1930 mL | 40.3861 mL | |
| 5 mM | 0.8077 mL | 4.0386 mL | 8.0772 mL | |
| 10 mM | 0.4039 mL | 2.0193 mL | 4.0386 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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