Home Transmembrane Transporters TRP Channel agonist - Taste Receptor inhibitor Probenecid For research use only.

Probenecid

Synonyms: Benemid

Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker.

Probenecid Chemical Structure

Probenecid Chemical Structure

CAS No. 57-66-9

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Probenecid Related Products

Biological Activity

Description Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker.
Targets
organic anion transport [1] TRPV2 [2] TAS2R16 [4]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04939623 Recruiting
Chronic Pain|Drug Dependence of Morphine Type|Symptom Withdrawal
University of Calgary
 October 31 2023 Phase 2
NCT05497674 Completed
Type 2 Diabetes Mellitus
Sunshine Lake Pharma Co. Ltd.
 February 21 2022 Phase 1
NCT05082909 Unknown status
Infection Bacterial
Imperial College London
 December 21 2021 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 285.36 Formula

C13H19NO4S
CAS No. 57-66-9 SDF Download Probenecid SDF
Smiles CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (199.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble


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In vivo
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