Catalog No.S4022

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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Probenecid  Chemical Structure

Probenecid Chemical Structure
Molecular Weight: 285.36

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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.
Targets TRPV2 hTAS2R16 hTAS2R38
IC50 31.9 μM (EC50) [2] 292 μM [4] 211 μM [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]

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Chemical Information

Download Probenecid SDF
Molecular Weight (MW) 285.36


CAS No. 57-66-9
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms Probalan
Solubility (25°C) * In vitro DMSO 57 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol 22 mg/mL (77 mM)
* <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 Name Benzoic acid, 4-[(dipropylamino)sulfonyl]-

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.28536 2.8536 5.7072 8.5608

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