Kynurenic acid
Based on 11 publication(s) in Google Scholar
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.
- Purity: 99.93%
- CAS No.: 492-27-3
- Formula: C10H7NO3
- Molecular Weight:189.17
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Kynurenic acid
More- Immunity. 2025 Sep 9;58(9):2320-2335.e9. [Abstract]
- Nat Metab. 2023 Feb;5(2):331-348. [Abstract]
- Neuron. 2026 Mar 26:S0896-6273(26)00120-0. [Abstract]
- Mol Metab. 2026 Jun 18:110:102403. [Abstract]
- Antioxidants (Basel). 2026 Feb 27;15(3):300. [Abstract]
- J Anim Sci Biotechnol. 2023 Aug 5;14(1):111. [Abstract]
- Cell Prolif. 2025 Jun;58(6):e13816. [Abstract]
- Int Immunopharmacol. 2024 Dec 31:147:113651. [Abstract]
- Sci Hortic. 2025 Dec 11;355:114551.
- In Vitro Cell Dev Biol Anim. 2023 May;59(5):356-365. [Abstract]
- Res Sq. 2025 Apr 08.
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Flow Cytometry
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
All iGluR Isoforms
MoreAll Endogenous Metabolite Isoforms
More
Biological Activity
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Human Endogenous Metabolite |
NMDA Receptor |
GPR35 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
217 μM
Compound: 1
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Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
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[PMID: 23713606] |
| CHO | EC50 |
39.2 μM
Compound: 1
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Agonist activity at human GPR35 expressed in CHO cells assessed as increase in intracellular Ca2+ measured over 20 secs by Aequorin assay
Agonist activity at human GPR35 expressed in CHO cells assessed as increase in intracellular Ca2+ measured over 20 secs by Aequorin assay
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[PMID: 23888932] |
| CHO | EC50 |
66 μM
Compound: 1
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Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
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[PMID: 23713606] |
| HT-29 | EC50 |
152 μM
Compound: Kynurenic acid
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Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assay
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[PMID: 22572579] |
| U2OS | EC50 |
>500 μM
Compound: Kynurenic acid
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Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation after 5 hrs by Tango assay
Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation after 5 hrs by Tango assay
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[PMID: 22572579] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 492-27-3
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Appearance Solid
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Molecular Weight 189.17
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Formula C10H7NO3
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Color Off-white to light yellow
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SMILES
O=C(C1=NC2=CC=CC=C2C(O)=C1)O
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Synonyms
Quinurenic acid
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Immunity
Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452 -
Nat Metab
2023 Feb;5(2):331-348. PMID: 36782071
Kynurenic acid purchased from MedChemExpress. Usage Cited in: Nat Metab. 2023 Feb;5(2):331-348. [Abstract]
The correlation heat map revealed that TPN-induced depletion of Lactobacillaceae and Muribaculum was positively correlated with the levels of IAA, ILA, indole and Kynurenic acid, while TPN-induced enrichment of Akkermansia, Helicobacter and Oscilibacter was negatively associated with indole metabolites.
Kynurenic acid purchased from MedChemExpress. Usage Cited in: Nat Metab. 2023 Feb;5(2):331-348. [Abstract]
After administration of Kynurenic acid to a TPN mouse model, the blood concentration of kynurenic acid at the samples harvest time point.
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Neuron
Dual anterior insula-prefrontal cortex circuits mediate chronic stress-induced social interaction deficits. [Abstract]2026 Mar 26:S0896-6273(26)00120-0. PMID: 41895265 -
Mol Metab
2026 Jun 18:110:102403. PMID: 42314903 -
Antioxidants (Basel)
Kynurenic Acid/GPR35 Signaling Protects the Infarcted Heart by Suppressing Macrophage mtDNA-Triggered cGAS-STING Activation. [Abstract]2026 Feb 27;15(3):300. PMID: 41897447 -
J Anim Sci Biotechnol
2023 Aug 5;14(1):111. PMID: 37542282 -
Cell Prolif
Tryptophan Metabolic Enzyme IL4I1 Inhibits Ferroptosis by Decreasing Ubiquitination of Nrf2 via I3P in Glioblastoma. [Abstract]2025 Jun;58(6):e13816. PMID: 40071723 -
Int Immunopharmacol
The tryptophan metabolite kynurenic acid ameliorates septic colonic injury through activation of the PPARγ signaling pathway. [Abstract]2024 Dec 31:147:113651. PMID: 39742725
Kynurenic acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 Dec 31:147:113651. [Abstract]
Following KYNA (100 μM, 4 h) treatment, the expression level of CD206 in M1 macrophages was significantly upregulated, indicating that KYNA can indeed promote the transformation of M1 macrophages into M2 macrophages.
Kynurenic acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 Dec 31:147:113651. [Abstract]
A comparison of the colon lengths among the five groups revealed that KYNA (1.5-2.5 mg/kg) intervention slightly improved the colon lengths of the mice.
Kynurenic acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 Dec 31:147:113651. [Abstract]
The presence of KYNA (0.5-2.5 mg/kg) led to a reduction in colon damage, restoration of mucosal integrity, and its protective effect increased with higher dosages.
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In Vitro Cell Dev Biol Anim
2023 May;59(5):356-365. PMID: 37291335 -
Solvent & Solubility
0.1 M NaOH : 12.5 mg/mL (66.08 mM; ultrasonic and adjust pH to 9 with NaOH)
DMSO : 8.75 mg/mL (46.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 33.33 mg/mL (176.19 mM); Suspended solution; Need ultrasonic
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang J, et al. Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35. J Biol Chem. 2006 Aug 4;281(31):22021-8. [Content Brief]
[2]. Albuquerque EX, et al. Kynurenic acid as an antagonist of α7 nicotinic acetylcholine receptors in the brain: facts and challenges. Biochem Pharmacol. 2013 Apr 15;85(8):1027-32. [Content Brief]
[3]. Małaczewska J, et al. Effect of oral administration of kynurenic acid on the activity of the peripheral blood leukocytes in mice. Cent Eur J Immunol. 2014;39(1):6-13. [Content Brief]
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 |