1. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation GPCR/G Protein
  2. iGluR Endogenous Metabolite Apoptosis CXCR GPR35
  3. Kynurenic acid

Kynurenic acid  (Synonyms: Quinurenic acid)

Cat. No.: HY-100806 Purity: 99.58%
COA Handling Instructions

Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

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

Kynurenic acid Chemical Structure

Kynurenic acid Chemical Structure

CAS No. : 492-27-3

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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

IC50 & Target[1]

Human Endogenous Metabolite

 

NMDA Receptor

 

GPR35

 

In Vitro

GPR35 functions as a receptor for the kynurenine pathway intermediate kynurenic acid. Kynurenic acid elicits calcium mobilization and inositol phosphate production in a GPR35-dependent manner in the presence of G qi/o chimeric G proteins. Kynurenic acid stimulates [35S]guanosine 5′-O-(3-thiotriphosphate) binding in GPR35-expressing cells, an effect abolished by pertussis toxin treatment. Kynurenic acid also induces the internalization of GPR35[1]. KYNA’s neuroinhibitory qualities and its neuroprotective and anticonvulsant effects are discovered using concentrations of the compound in the millimolar range. This, as well as the low affinity of KYNA at each of the three ionotropic glutamate receptors responsible for these effects [NMDA, alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) and kainate], together with the realization that KYNA concentrations in the mammalian brain are in the sub-micromolar range, suggested that other receptors might serve as targets of endogenous Kynurenic acid. Kynurenic acid, with a shallower inhibition curve and non-competitively, antagonizes α7nAChRs on cultured hippocampal neurons with an IC50 in the low micromolar range[2].

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

In Vivo

Kynurenic acid affects the activity of leukocytes in the peripheral blood of mice, although the lowest one (2.5 mg/L) has the most profound influence in contrast to the highest one (250 mg/L), which produces the weakest effect. The lowest Kynurenic acid dose stimulates the proliferative response of T lymphocytes (p<0.05), after 7 and 28 days of administering the acid to the animals[3].

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

Clinical Trial
Molecular Weight

189.17

Formula

C10H7NO3

CAS No.
Unlabeled CAS

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC2=CC=CC=C2C(O)=C1)O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

0.1 M NaOH : 12.5 mg/mL (66.08 mM; ultrasonic and adjust pH to 9 with NaOH)

DMSO : 9 mg/mL (47.58 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.2863 mL 26.4313 mL 52.8625 mL
5 mM 1.0573 mL 5.2863 mL 10.5725 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 1.25 mg/mL (6.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (6.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 33.33 mg/mL (176.19 mM); Suspended solution; Need ultrasonic

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
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).
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.
Purity & Documentation

Purity: 99.58%

References
Kinase Assay
[1]

CHO-GPR35 stable cells are pretreated with or without pertussis toxin (100 ng/mL) for 16 h before harvesting. Cells are resuspended and homogenized in 10 mM Tris-HCl (pH 7.4), 1 mM EDTA followed by centrifugation at 1000 ×g for 10 min at 4 °C to remove nuclei and cellular debris. Membrane fractions are collected by spinning the supernatant at 38,000 ×g for 30 min and resuspended in 20 mM HEPES (pH 7.5) and 5 mM MgCl2. 25 μg of membranes is incubated at room temperature for 1 h in assay buffer (20 mM HEPES, 5 m MMgCl2, 0.1% bovine serum albumin (pH 7.5)) containing 3 μM GDP and 0.1 nM[35S]GTPγS in the absence or presence of kynurenic acid. Reactions are terminated by vacuum filtration through GF/B filters, and the retained radioactivities are quantified on liquid scintillation counter[1].

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

Animal Administration
[3]

Mouse: The experiment is performed on 160 male BALB/c mice, aged 10-12 weeks, with body weight of 22-26 g. The animals are maintained on a 12-h light/dark cycle at controlled temperature (20 ±1°C) and supplied with rodent chow and water ad libitum throughout the experiment. Mice are divided randomLy into four equal groups: control group (0) not receiving the Kynurenic acid, and three experimental groups administered the Kynurenic acid solution in drinking water at concentrations of 2.5, 25 or 250 mg/L. After 3, 7, 14 and 28 consecutive days of administration of the Kynurenic acid solution, 10 individuals from each group are sacrificed. The animals are anesthetized by inhalation of Aerrane and their blood is collected by heart puncture. Blood collected from five individuals of each group is used for the MTT assay, and from the next five for the flow cytometry[3].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / 0.1 M NaOH 1 mM 5.2863 mL 26.4313 mL 52.8625 mL 132.1563 mL
5 mM 1.0573 mL 5.2863 mL 10.5725 mL 26.4313 mL
10 mM 0.5286 mL 2.6431 mL 5.2863 mL 13.2156 mL
15 mM 0.3524 mL 1.7621 mL 3.5242 mL 8.8104 mL
20 mM 0.2643 mL 1.3216 mL 2.6431 mL 6.6078 mL
25 mM 0.2115 mL 1.0573 mL 2.1145 mL 5.2863 mL
30 mM 0.1762 mL 0.8810 mL 1.7621 mL 4.4052 mL
40 mM 0.1322 mL 0.6608 mL 1.3216 mL 3.3039 mL
0.1 M NaOH 50 mM 0.1057 mL 0.5286 mL 1.0573 mL 2.6431 mL
60 mM 0.0881 mL 0.4405 mL 0.8810 mL 2.2026 mL
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  • Do most proteins show cross-species activity?

    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.

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