For research use only.
Catalog No.S4022 Synonyms: Benemid
Molecular Weight(MW): 285.36
Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16.
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|Description||Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16.|
Probenecid is able to prevent the efflux of calcium-sensitive fluorescent dyes during studies of cellular calcium mobilization. Probenecid (2.5 mM) is found to block the export of Fura-2 from 1321N1 astrocytoma cells, and does not change the basal calcium concentration or the muscarinic calcium response.  Probenecid is a potent transient receptor potential vanilloid 2 (TRPV2) agonist. Probenecid selectively induces increase in intracellular Ca2+ influx in HEK293T cells transiently expressing exogenous TRPV2.  Probenecid is able to interact with organic anion transporters (OAT). 0.1 mM Probenecid efficiently inhibits ATP-dependent active vesicular N-ethylmaleimide glutathione (NEM-GS) uptake by Human Multidrug Resistance Proteins 1 (MRP1) and MRP2. In isolated Sf9 cell membranes, Probenecid stimulates ATPase activity of MRP2 with approximate KACT of 250 μM, but inhibits ATPase activity of MRP1.  Probenecid is an inhibitor of the hTAS2R16, hTAS2R38, and hTAS2R43 bitter taste receptors. 1 mM Probenecid attenuates saccharin-induced calcium flux responses of hTAS2R16 to near baseline levels. Probenecid dose-dependently inhibits hTAS2R16 (in the presence of 3 mM salicin) and hTAS2R38 (in the presence of 300 μM PTC). This activity is independent of Probenecid's activity as a transport inhibitor, but is concerning with Probenecid interaction with the receptor. 
|In vivo||Probenecid is an inhibitor of organic transport in vivo. Probenecid is able to decrease the renal clearance of antibiotic, such as penicillin, which enhances serum levels of antibiotic. Probenecid enhances the renal excretion of urate by acting as a competitive inhibitor of OAT, which prevents OAT-mediated reuptake of uric acid from the urine to the serum. Probenecid is found to block acid metabolites from exiting the central nervous system, and is a competitive inhibitor of monoamine transport in the kidney, liver, and the eye. |
|In vitro||DMSO||57 mg/mL (199.74 mM)|
|Ethanol||22 mg/mL (77.09 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01428284||Completed||Drug: Canagliflozin/Probenecid||Healthy||Johnson & Johnson Pharmaceutical Research & Development L.L.C.||August 2011||Phase 1|
|NCT00690014||Completed||Drug: probenecid||Kidney Disease||University of Maryland College Park|National Institutes of Health (NIH)|National Institute of General Medical Sciences (NIGMS)|University of Maryland Baltimore||August 2006||Not Applicable|
|NCT00304434||Completed||Drug: Oseltamivir|Drug: Probenecid||Influenza||US Department of Veterans Affairs|Brooke Army Medical Center|National Institutes of Health (NIH)|VA Office of Research and Development||February 2005||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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