| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Indoxyl sulfate-d4 potassium shares the same molecular target as its non-deuterated form, indoxyl sulfate. Indoxyl sulfate is a potent endogenous agonist for the human aryl hydrocarbon receptor (AhR). AhR is a ligand-activated transcription factor involved in the regulation of xenobiotic metabolism, immune responses, and cell proliferation. Indoxyl sulfate also activates the organic anion transporters (OAT1 and OAT3) for its renal uptake and secretion. The labeled compound is used as a tracer to study the metabolism and biological activity of indoxyl sulfate.
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| 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 effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
The deuterated compound itself does not possess intrinsic pharmacological activity in vitro; its biological activity is identical to that of indoxyl sulfate. Indoxyl sulfate is a uremic toxin that accumulates in the blood of patients with chronic kidney disease (CKD). In vitro studies have shown that indoxyl sulfate induces oxidative stress, activates the NF-κB pathway, and promotes the expression of pro-inflammatory and pro-fibrotic genes in renal tubular cells. It also inhibits endothelial cell proliferation and angiogenesis. The labeled compound is used as an internal standard for quantifying indoxyl sulfate in biological samples. |
| ln Vivo |
Indoxyl sulfate-d4 potassium is not used as a therapeutic agent; its non-deuterated form, indoxyl sulfate, is a uremic toxin that accumulates in CKD patients and contributes to the progression of kidney disease, cardiovascular disease, and bone disorders. In vivo, indoxyl sulfate is produced from tryptophan by gut microbiota and is normally excreted in urine. In CKD, it accumulates in the blood. The labeled compound is used in pharmacokinetic and metabolic studies to accurately measure indoxyl sulfate levels in plasma, urine, and tissue samples.
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| Enzyme Assay |
In vitro assays for indoxyl sulfate-d4 potassium focus on its use as an analytical standard rather than a receptor-binding agent. A standard protocol for uremic toxin analysis involves preparing a solution of the compound in an appropriate solvent (e.g., methanol or water) and using it as an internal standard for LC-MS/MS analysis. The compound is added to biological samples (e.g., serum, urine, or tissue homogenates) before extraction and cleanup procedures. Quantification is performed by monitoring specific mass transitions for the labeled and unlabeled compounds. Quality control includes purity analysis (>95%).
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| Cell Assay |
In vitro cell culture experiments are not performed with indoxyl sulfate-d4 potassium. When studying the effects of indoxyl sulfate in cellular systems, the non-labeled compound is used. Renal tubular cells (e.g., HK-2 or NRK-52E cells) are treated with indoxyl sulfate at concentrations ranging from 10 to 1000 µM, and oxidative stress, inflammation, and fibrosis markers are measured. The labeled compound is used as an internal standard for LC-MS/MS analysis of indoxyl sulfate concentrations in cell culture media or lysates.
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| Animal Protocol |
In vivo animal studies are not conducted with indoxyl sulfate-d4 potassium. When used in pharmacokinetic studies, the labeled compound serves as an internal standard for the quantification of indoxyl sulfate in animal plasma or tissue samples. In typical protocols, animals (e.g., rats with induced CKD) are monitored for indoxyl sulfate accumulation. The labeled internal standard is added to the samples before analysis by LC-MS/MS to ensure accurate and precise quantification.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of indoxyl sulfate-d4 potassium itself are not characterized, as it is not a drug substance. Indoxyl sulfate is produced endogenously from tryptophan by gut microbiota and is normally excreted in urine by organic anion transporters (OAT1 and OAT3). In CKD patients, plasma levels of indoxyl sulfate are significantly elevated due to impaired renal clearance. The labeled compound is used as an internal standard to accurately quantify indoxyl sulfate in pharmacokinetic and biomonitoring studies.
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| Toxicity/Toxicokinetics |
Indoxyl sulfate-d4 potassium is not a therapeutic agent and has not been evaluated for toxicity in humans. Its non-deuterated form, indoxyl sulfate, is a uremic toxin that contributes to the progression of CKD and its complications. High levels of indoxyl sulfate are associated with increased oxidative stress, inflammation, and cardiovascular disease in CKD patients. The labeled compound is for research use only and should be handled with standard laboratory precautions.
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| References | |
| Additional Infomation |
Indoxyl sulfate-d4 potassium is a stable isotope-labeled internal standard used in studies of uremic toxins and kidney disease biomarkers. It is also known as 3-indoxyl sulfate-d4 potassium salt. The compound is used in analytical method development, quality control, and biomonitoring studies. The incorporation of deuterium allows for accurate quantification of indoxyl sulfate in biological samples using mass spectrometry.
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| Molecular Formula |
C8H2D4KNO4S
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|---|---|
| Molecular Weight |
255.33
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| Exact Mass |
254.99
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| CAS # |
1346601-03-3
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| Related CAS # |
Potassium 1H-indol-3-yl sulfate;2642-37-7
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| PubChem CID |
5177095
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
302
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MDAWATNFDJIBBD-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C8H7NO4S.K/c10-14(11,12)13-8-5-9-7-4-2-1-3-6(7)8;/h1-5,9H,(H,10,11,12);/q;+1/p-1
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| Chemical Name |
potassium;1H-indol-3-yl sulfate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.9165 mL | 19.5825 mL | 39.1650 mL | |
| 5 mM | 0.7833 mL | 3.9165 mL | 7.8330 mL | |
| 10 mM | 0.3917 mL | 1.9583 mL | 3.9165 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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