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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock

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Biological Activity

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 <1 mg/mL

* 1 mg/ml means slightly soluble or 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02243631 Recruiting Calcium Pyrophosphate Deposition Disease VA Office of Research and Development October 2014 Early Phase 1
NCT01937026 Completed Healthy Volunteers Eli Lilly and Company September 2013 Phase 1
NCT01816646 Completed Blood And Marrow Transplantation M.D. Anderson Cancer Center|Gilead Sciences September 2013 Phase 1
NCT01814319 Completed Systolic Heart Failure University of Cincinnati March 2013 Phase 2
NCT01634100 Completed Healthy Boehringer Ingelheim June 2012 Phase 1
NCT01428284 Completed Healthy Johnson & Johnson Pharmaceutical Research & Development, L.L.C. August 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID