For research use only.

Catalog No.S4022 Synonyms: Benemid

Probenecid  Chemical Structure

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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10mM (1mL in DMSO) USD 130 In stock
USD 97 In stock
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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.
organic anion transport [1]
TRPV2 [2]
TAS2R16 [4]
In vitro

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. [1] 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. [2] 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. [3] 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. [4]

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. [5]


Solubility (25°C)

In vitro DMSO 57 mg/mL (199.74 mM)
Ethanol 22 mg/mL (77.09 mM)
Water Insoluble

* 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.

Chemical Information

Molecular Weight 285.36


CAS No. 57-66-9
Storage powder
in solvent
Synonyms Benemid
Smiles CCCN(CCC)[S](=O)(=O)C1=CC=C(C=C1)C(O)=O

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID