2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. 5,7-Dichlorokynurenic acid

5,7-Dichlorokynurenic acid  (Synonyms: 5,7-DCKA)

製品番号: HY-100834 純度: 99.98%
COA 取扱説明書 Technical Support

5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission.

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5,7-Dichlorokynurenic acid

5,7-Dichlorokynurenic acid 構造式

CAS 番号 : 131123-76-7

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $85 在庫あり
25 mg $185 在庫あり
50 mg $315 在庫あり
100 mg $470 在庫あり
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Based on 1 publication(s) in Google Scholar

Other Forms of 5,7-Dichlorokynurenic acid:

5,7-Dichlorokynurenic acid 関連抗体

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AMPA Receptor NMDA Receptor Kainate Receptor

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製品説明

5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission[1][2].

IC50 & Target

NMDA Receptor

 

体外実験

5,7-dichlorokynurenic acid (0.2-400 μM) is a potent, competitive antagonist of the glycine site on NMDA receptors expressed in rat brain mRNA-injected Xenopus oocytes, with a KB of 65 nM, and is 509-fold more selective for this site than for kainate receptors[1].
5,7-dichlorokynurenic acid (40 nM-10 μM; 60 min on ice) potently displaces [3H]glycine from strychnine-insensitive glycine sites on rat brain cortex membranes with a Ki of 40 nM, and does not bind to the NMDA recognition site at 10 μM[1].
5,7-dichlorokynurenic acid (1-10 μM) reduces NMDA-induced neuronal injury in primary rat cortical cell cultures, with 1 μM yielding 55-79% protection and 10 μM yielding 62-90% protection[1].

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

5,7-Dichlorokynurenic acid 関連抗体
体内実験

5,7-Dichlorokynurenic acid (30.0-100.0 mg/kg; i.p.; single dose) produces anxiolytic-like effects in the social interaction model, increasing social interaction time by +37% at 30.0 mg/kg and +32% at 100.0 mg/kg, with reduced motor activity at the highest dose[2].
5,7-Dichlorokynurenic acid (100.0 mg/kg; i.p.; single dose) produces anxiolytic-like effects in the elevated plus maze model, increasing open arm exploration time by +41% at 100.0 mg/kg, with reduced motor activity[2].
5,7-Dichlorokynurenic acid (100.0-173.0 mg/kg; i.p.; single dose) disinhibits suppressed conflict responding in the Cook and Davidson conditioned anxiety model at 100.0 mg/kg and 173.0 mg/kg without altering non-punished responding[2].
5,7-Dichlorokynurenic acid (10.0-100.0 mg/kg; i.p.; single dose) does not generalize to the MK-801 discriminative cue at 10.0 mg/kg, and shows minimal partial generalization in 1 of 4 rats at 100.0 mg/kg[2].

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

Animal Model: Wistar rats (male, 200-300 g)[2]
Dosage: 30.0 mg/kg; 100.0 mg/kg
Administration: i.p.; single dose
Result: Increased social interaction time significantly by +37% with no significant change in motor activity at 30.0 mg/kg.
Increased social interaction time significantly by +32%, and decreased motor activity significantly by -34% at 100.0 mg/kg.
分子量

258.06

分子式

C10H5Cl2NO3
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=NC2=CC(Cl)=CC(Cl)=C2C(O)=C1)O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 25 mg/mL (96.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8751 mL 19.3753 mL 38.7507 mL
5 mM 0.7750 mL 3.8751 mL 7.7501 mL
10 mM 0.3875 mL 1.9375 mL 3.8751 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

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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: ≥ 2.5 mg/mL (9.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.
純度とドキュメンテーション

純度: 99.98%

COA (249 KB) HNMR (139 KB) RP-HPLC (167 KB) LCMS (105 KB)

取扱説明書 (2659 KB)
参考文献

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 (sealed storage, away from moisture). 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
DMSO 1 mM 3.8751 mL 19.3753 mL 38.7507 mL 96.8767 mL
5 mM 0.7750 mL 3.8751 mL 7.7501 mL 19.3753 mL
10 mM 0.3875 mL 1.9375 mL 3.8751 mL 9.6877 mL
15 mM 0.2583 mL 1.2917 mL 2.5834 mL 6.4584 mL
20 mM 0.1938 mL 0.9688 mL 1.9375 mL 4.8438 mL
25 mM 0.1550 mL 0.7750 mL 1.5500 mL 3.8751 mL
30 mM 0.1292 mL 0.6458 mL 1.2917 mL 3.2292 mL
40 mM 0.0969 mL 0.4844 mL 0.9688 mL 2.4219 mL
50 mM 0.0775 mL 0.3875 mL 0.7750 mL 1.9375 mL
60 mM 0.0646 mL 0.3229 mL 0.6458 mL 1.6146 mL
80 mM 0.0484 mL 0.2422 mL 0.4844 mL 1.2110 mL
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5,7-Dichlorokynurenic acid Related Classifications

  • Molarity Calculator

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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    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:

5,7-Dichlorokynurenic acid131123-76-75,7-DCKAiGluRIonotropic glutamate receptorsrat brain cortex membranesneuron injurysocial interaction modelkainate receptorratrodent modelsXenopus oocytesglycine site NMDA receptorprimary rat cortical cell culturesanxietyInhibitorinhibitorinhibit

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