| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Etebenecid shares a similar mechanism of action with other sulfonamide-based uricosurics like probenecid. It functions as an inhibitor of organic anion transporters and certain ATP-binding cassette (ABC) transporters. This inhibition modulates cellular drug efflux and metabolite transport. By inhibiting renal tubular reabsorption of uric acid and organic anions, etebenecid promotes their excretion.
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| ln Vitro |
In vitro studies of etebenecid are primarily focused on its role as a transporter inhibitor. Its activity can be assessed using cell-based uptake assays where cells expressing specific organic anion transporters (OATs) or ABC transporters are incubated with a fluorescent or radiolabeled substrate in the presence of varying concentrations of etebenecid. The inhibition of substrate uptake is quantified to determine the IC₅₀ for transporter inhibition.
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| ln Vivo |
Etebenecid is not typically used as a therapeutic agent in vivo. Its primary application is as a research tool to study transporter function and drug-drug interactions. In animal models, it can be administered to modulate the pharmacokinetics of other compounds that are substrates of organic anion transporters, thereby altering their tissue distribution and elimination.
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| Enzyme Assay |
Non-cellular enzyme assays for etebenecid are limited as it acts on transporters rather than enzymes. Its binding affinity for organic anion transporters can be assessed using membrane vesicle preparations. Membrane vesicles containing the transporter of interest are incubated with a radiolabeled substrate and varying concentrations of etebenecid. The amount of substrate transported into the vesicles is measured, and the IC₅₀ for inhibition is determined.
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| Cell Assay |
In vitro cellular assays for etebenecid involve treating cells that overexpress specific organic anion transporters (e.g., OAT1, OAT3) or ABC transporters (e.g., MRP4) with the compound. Cells are incubated with a fluorescent or radiolabeled substrate (e.g., para-aminohippurate, methotrexate) in the presence of varying concentrations of etebenecid. The intracellular accumulation of the substrate is measured, and the IC₅₀ for inhibition of transport is determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments with etebenecid are conducted to study its effects on the pharmacokinetics of other drugs. Rodents are co-administered etebenecid with a substrate drug that is eliminated via organic anion transporters. Blood and tissue samples are collected at various time points, and the concentrations of the substrate drug are measured. The effect of etebenecid on the substrate's pharmacokinetic parameters (e.g., AUC, half-life, clearance) is assessed.
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| ADME/Pharmacokinetics |
Etebenecid has a molecular weight of 287.34 and a molecular formula of C₁₁H₁₅NO₄S. It is a solid powder with a purity of ≥98%. The compound is typically stored at room temperature in a dry place. It is soluble in organic solvents such as DMSO. Detailed pharmacokinetic parameters for etebenecid itself are not extensively characterized, as it is primarily a research tool.
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| Toxicity/Toxicokinetics |
Etebenecid is generally considered to have a favorable tolerability profile compared to probenecid, as it causes fewer gastrointestinal side effects. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation. Appropriate personal protective equipment should be used.
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| Additional Infomation |
Etebenecid is a sulfonamide drug.
Etebenecid (CAS 1213-06-5) is a probenecid analog and a pharmacological tool used to inhibit organic anion transporters and ABC transporters. It functions as a uricosuric agent and is used in research to study drug transport, renal excretion, and drug-drug interactions. Its improved gastrointestinal tolerability compared to probenecid makes it a valuable alternative for specific research applications. |
| Molecular Formula |
C11H15NO4S
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|---|---|
| Molecular Weight |
257.3
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| Exact Mass |
257.072
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| CAS # |
1213-06-5
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| PubChem CID |
14604
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.283g/cm3
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| Boiling Point |
416.5ºC at 760mmHg
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| Flash Point |
205.7ºC
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| Vapour Pressure |
1.11E-07mmHg at 25°C
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| LogP |
2.496
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
17
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| Complexity |
348
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O)C1=CC=C(S(=O)(N(CC)CC)=O)C=C1
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| InChi Key |
UACOQEQOBAQRDQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H15NO4S/c1-3-12(4-2)17(15,16)10-7-5-9(6-8-10)11(13)14/h5-8H,3-4H2,1-2H3,(H,13,14)
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| Chemical Name |
4-(diethylsulfamoyl)benzoic acid
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| Synonyms |
NSC 49467; Etebenecid; Etebenecidum
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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 : ~250 mg/mL (~971.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.08 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 20.8 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: ≥ 2.08 mg/mL (8.08 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 20.8 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: ≥ 2.08 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8865 mL | 19.4326 mL | 38.8651 mL | |
| 5 mM | 0.7773 mL | 3.8865 mL | 7.7730 mL | |
| 10 mM | 0.3887 mL | 1.9433 mL | 3.8865 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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