| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
NMDA receptor glycine site (glycineB site). DCKA is a selective competitive antagonist at the glycine modulatory site of the NMDA receptor, with a Kb of 65 nM. In radioligand binding assays, DCKA has a Ki of 40 nM. It selectively inhibits glycine- over kainate-induced NMDA currents at 15 μM.
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| ln Vitro |
DCKA reduces NMDA-induced neurotoxicity in primary rat cortical neurons by 55 to 90% when used at concentrations ranging from 1 to 10 μM. It protects against excitotoxicity-induced neuronal damage. In Xenopus oocytes expressing rat NMDA receptors, DCKA selectively inhibits glycine- over kainate-induced NMDA currents at 15 μM.
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| ln Vivo |
In vivo, DCKA (0.97-97 nmol) reverses mechanical hyperalgesia in magnesium-deficient rats in a dose-dependent manner. It blocks the positive ionotropic effect, hypertension, and increase in myocardial oxygen demand induced by electrical stimulation of the paraventricular nucleus (PVN) in anesthetized rabbits. DCKA also reduces the severity of seizures in animal models.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for DCKA typically involve radioligand binding studies using rat brain membrane preparations or cells expressing recombinant NMDA receptors. Membranes are incubated with a radiolabeled glycine site ligand (such as [3H]MDL-105,519 or [3H]glycine) in the presence of varying concentrations of DCKA. Non-specific binding is determined using excess unlabeled glycine or a selective glycine site antagonist. Bound radioactivity is measured by filtration and scintillation counting to calculate Ki or IC50 values.
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| Cell Assay |
In vitro cellular assays are performed using primary neuronal cultures, typically rat cortical or hippocampal neurons. Cells are exposed to NMDA and glycine in the presence of DCKA, and neurotoxicity is assessed by measuring cell viability (e.g., LDH release, MTT assay) or intracellular calcium levels. Electrophysiological studies using patch-clamp or two-electrode voltage-clamp in Xenopus oocytes expressing recombinant NMDA receptors can also be performed to measure DCKA's effects on NMDA-induced currents.
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| Animal Protocol |
In vivo animal studies typically utilize rodent models. For analgesia studies, magnesium-deficient rats are administered DCKA via intrathecal or intracerebroventricular injection (0.97-97 nmol), and mechanical hyperalgesia is assessed using von Frey filaments or paw withdrawal tests. In seizure models, DCKA is administered prior to chemoconvulsant challenge, and seizure severity is scored. For cardiovascular studies, DCKA is administered to anesthetized rabbits, and hemodynamic parameters are monitored.
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| ADME/Pharmacokinetics |
DCKA has a molecular weight of 258.05 g/mol and molecular formula C10H5Cl2NO3. It is a crystalline solid with purity ≥98%. DCKA is soluble in DMSO and should be stored at -20°C. The compound has UV absorbance maxima at 228, 256, and 342 nm. It is stable for ≥4 years when stored properly.
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| Toxicity/Toxicokinetics |
DCKA has been shown to have potential therapeutic applications in various neurological and psychiatric disorders, but may also have potential toxic effects. Standard laboratory safety precautions should be followed when handling DCKA. The compound is for research use only and not for therapeutic or veterinary use. No specific acute toxicity data have been reported in the literature.
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| References | |
| Additional Infomation |
5,7-Dichloro-4-oxo-1H-quinoline-2-carboxylic acid is a member of the quinoline class of compounds.
DCKA is a kynurenic acid derivative and a potent antagonist of the NMDA receptor glycine site. It has been extensively studied for its potential therapeutic applications in neurological and psychiatric disorders such as schizophrenia, depression, and Alzheimer's disease. DCKA is also used to study the role of NMDA receptor glycine site in synaptic plasticity, learning, and memory processes. The compound is for research use only and has not been approved for clinical use. |
| Molecular Formula |
C10H5CL2NO3
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|---|---|
| Molecular Weight |
258.05
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| Exact Mass |
256.965
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| CAS # |
131123-76-7
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| PubChem CID |
1779
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.945
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| Hydrogen Bond Donor Count |
2
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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 |
369
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BGKFPRIGXAVYNX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H5Cl2NO3/c11-4-1-5(12)9-6(2-4)13-7(10(15)16)3-8(9)14/h1-3H,(H,13,14)(H,15,16)
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| Chemical Name |
5,7-dichloro-4-oxo-1H-quinoline-2-carboxylic acid
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| Synonyms |
DKC; DCKA
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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, 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) |
DMSO : ~25 mg/mL (~96.88 mM)
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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 | 3.8752 mL | 19.3761 mL | 38.7522 mL | |
| 5 mM | 0.7750 mL | 3.8752 mL | 7.7504 mL | |
| 10 mM | 0.3875 mL | 1.9376 mL | 3.8752 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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