| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Indoxyl sulfate is an agonist for the aryl hydrocarbon receptor (AhR), a key regulator of immune-inflammatory conditions. It is also a substrate for organic anion transporters (OAT1 and OAT3) in renal proximal tubules, which mediate its secretion and accumulation in chronic kidney disease.
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|---|---|
| ln Vitro |
In vitro, indoxyl sulfate (250 microM) induces oxidative stress, inflammation, and fibrosis in cultured renal tubular cells (HK-2) and human endothelial cells. It inhibits endothelial proliferation and migration, and promotes the expression of pro-inflammatory cytokines (IL-6, TNF-alpha) via AhR activation.
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| ln Vivo |
In chronic kidney disease (CKD) patients with impaired renal function, indoxyl sulfate accumulates in serum as a uremic toxin, inducing oxidative stress and accelerating disease progression. In animal models (5/6 nephrectomy rats), elevated indoxyl sulfate levels correlate with renal fibrosis progression.
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| Enzyme Assay |
A non-cell assay for AhR activation is performed using a luciferase reporter gene assay. HEK293 cells are transiently transfected with an AhR-responsive luciferase plasmid and an AhR expression plasmid. Potassium indoxyl sulfate is added, and luciferase activity is measured after 6-24 hours. EC₅0 values are typically in the low micromolar range.
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| Cell Assay |
Human renal proximal tubular cells (HK-2) or human endothelial cells (HUVEC) are treated with potassium indoxyl sulfate (50-500 microM) for 24-72 hours. Markers of oxidative stress (8-OHdG, ROS) are measured by fluorescent probes. Inflammation markers (IL-6, TNF-alpha) are measured by ELISA. Fibrosis markers (TGF-beta, collagen I) are measured by qPCR or Western blot.
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| Animal Protocol |
Animal studies are typically performed in the 5/6 nephrectomy rat model of chronic kidney disease. Rats undergo surgical reduction of renal mass, then potassium indoxyl sulfate is administered by intraperitoneal injection or added to drinking water. Blood is collected for indoxyl sulfate measurement by HPLC, and kidney tissue is analyzed for fibrosis and oxidative stress.
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| ADME/Pharmacokinetics |
Indoxyl sulfate binds extensively to plasma albumin (~90%) and is actively secreted into the urine by OAT1/OAT3 in healthy individuals. In chronic kidney disease (CKD), its plasma half-life is significantly prolonged (8-24 hours) due to reduced renal clearance. It accumulates to 50-200 microM in serum of CKD patients.
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| Toxicity/Toxicokinetics |
As a uremic toxin, indoxyl sulfate is directly toxic to renal tubular cells and vascular endothelium. It is associated with the progression of chronic kidney disease, cardiovascular disease, bone disorders (renal osteodystrophy), and cognitive dysfunction. The potassium salt has similar toxicity to the free acid form.
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| Additional Infomation |
See other relationships...
Potassium 1H-indol-3-yl sulfate is used as a standard for indoxyl sulfate quantification in clinical chemistry and research, particularly for monitoring uremic toxin levels in CKD patients. It is studied as a potential therapeutic target for reducing uremic toxicity, and as an AhR agonist in immunology research. |
| Molecular Formula |
C8H6KNO4S
|
|---|---|
| Molecular Weight |
251.30
|
| Exact Mass |
250.965
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| CAS # |
2642-37-7
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| Related CAS # |
Indoxyl sulfate-d4 potassium;1346601-03-3
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| PubChem CID |
5177095
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| Appearance |
White to light brown solid powder
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| Melting Point |
165 °C (dec.)(lit.)
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| LogP |
2.087
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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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| SMILES |
C1=CC=C2C(=C1)C(=CN2)OS(=O)(=O)[O-].[K+]
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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 |
| 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) |
DMSO :~100 mg/mL (~397.93 mM)
H2O :~50 mg/mL (~198.97 mM ) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.5 mg/mL (9.95 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (99.48 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9793 mL | 19.8965 mL | 39.7931 mL | |
| 5 mM | 0.7959 mL | 3.9793 mL | 7.9586 mL | |
| 10 mM | 0.3979 mL | 1.9897 mL | 3.9793 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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