| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
L-Kynurenine (and its labeled form) targets the aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor involved in xenobiotic metabolism, immune regulation, and inflammation. It also serves as a substrate for enzymes along the kynurenine pathway.
|
|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an impact on a drug's pharmacokinetics and metabolic profile, it has drawn attention [1].
L-Kynurenine is an aryl hydrocarbon receptor (AhR) agonist. L-Kynurenine-d4-1 is a stable isotope-labeled version used as a tracer to study the metabolism and signaling of kynurenine. |
| ln Vivo |
L-Kynurenine is a key metabolite of tryptophan, involved in immune modulation, neurobiology, and cancer biology. The deuterated version is used as a tracer to quantify these processes.
|
| Enzyme Assay |
Non-cell binding assays for L-Kynurenine-d4-1 are performed using purified aryl hydrocarbon receptor (AhR) protein. A TR-FRET (time-resolved fluorescence resonance energy transfer) or fluorescence polarization (FP) assay can be used. The assay uses a fluorescently labeled AhR ligand (e.g., a high-affinity agonist). L-Kynurenine-d4-1 (0.001-1000 microM) competes with the labeled ligand for binding to the AhR. The change in FP or TR-FRET signal is measured. The IC50 is calculated, and the Ki is determined.
|
| Cell Assay |
Cellular assays for L-Kynurenine-d4-1 are performed using cell lines that express AhR (e.g., HepG2, HeLa, or immune cells). Cells are seeded in 6-well or 96-well plates and treated with L-Kynurenine-d4-1 (0.1-1000 uM) for 6-24 hours. The expression of AhR target genes (e.g., CYP1A1, CYP1B1) is measured by qRT-PCR. Alternatively, the compound can be used to trace the kynurenine pathway. Cells are treated with L-Kynurenine-d4-1 (1-100 uM), and the production of downstream metabolites (e.g., kynurenic acid, 3-hydroxykynurenine, anthranilic acid, quinolinic acid) is measured by LC-MS/MS.
|
| Animal Protocol |
In vivo animal studies with L-Kynurenine-d4-1 are performed to study kynurenine metabolism and its role in disease. Mice or rats are administered L-Kynurenine-d4-1 via IP injection (10-100 mg/kg) or oral gavage (50-200 mg/kg). Blood is collected at various time points. Tissues (liver, kidney, brain) are harvested. The enrichment of the labeled compound and its metabolites is measured by LC-MS/MS.
|
| ADME/Pharmacokinetics |
L-Kynurenine-d4-1 hydrochloride (MW ~248.7) is a stable isotope-labeled metabolite. Its pharmacokinetics are not determined separately from the unlabeled compound. L-Kynurenine is rapidly cleared from the plasma (half-life ~30-60 minutes) and is metabolized by kynureninase and kynurenine aminotransferase.
|
| Toxicity/Toxicokinetics |
D4-kynurenine is used at tracer doses, which are safe. The unlabeled L-Kynurenine may have immunomodulatory effects, but toxicity at research doses is low.
|
| References | |
| Additional Infomation |
L-Kynurenine-d4-1 hydrochloride is a stable isotope-labeled research compound used as an internal standard for LC-MS/MS quantification of L-Kynurenine in biological samples. It is also used to study the kynurenine pathway (tryptophan metabolism). The product is for research use only.
|
| Molecular Formula |
C10H9D4CLN2O3
|
|---|---|
| Molecular Weight |
248.70
|
| Related CAS # |
L-Kynurenine;2922-83-0;L-Kynurenine-d4-1;194546-33-3
|
| Appearance |
Solid powder
|
| SMILES |
OC([C@@H](N)CC(C1=C(C([2H])=C([2H])C([2H])=C1[2H])N)=O)=O.[H]Cl
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O: ~20 mg/mL (~80.4 mM; with ultrasonication)
DMSO: ~12.5 mg/mL (~50.3 mM; with ultrasonication and warming by heating to 60°C) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (20.8 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 2.08 mg/mL (8.36 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 DMSO stock solution (20.8 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (8.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (20.8 mg/mL) to 900 μL of corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0209 mL | 20.1045 mL | 40.2091 mL | |
| 5 mM | 0.8042 mL | 4.0209 mL | 8.0418 mL | |
| 10 mM | 0.4021 mL | 2.0105 mL | 4.0209 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.