Probenecid

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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In DMSO USD 130 In stock
USD 97 In stock
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Probenecid  Chemical Structure

Probenecid Chemical Structure
Molecular Weight: 285.36

Validation & Quality Control

Quality Control & MSDS

Product Information

Product Description

Biological Activity

Description Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16.
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]
Features

Protocol(Only for Reference)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] McDonough PM, et al. Cell Calcium, 1989, 10(3), 171-180.

[2] Bang S, et al. Neurosci Lett, 2007, 425(2), 120-125.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-12-20)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02243631 Recruiting Calcium Pyrophosphate Deposition Disease Department of Veterans Affairs October 2014 Phase 0
NCT02243631 Recruiting Calcium Pyrophosphate Deposition Disease Department of Veterans Affairs October 2014 Phase 0
NCT01937026 Completed Healthy Volunteers Eli Lilly and Company September 2013 Phase 1
NCT01816646 Active, not recruiting Blood And Marrow Transplantation M.D. Anderson Cancer Center|Gilead Sciences September 2013 Phase 1
NCT01937026 Completed Healthy Volunteers Eli Lilly and Company September 2013 Phase 1

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Chemical Information

Download Probenecid SDF
Molecular Weight (MW) 285.36
Formula

C13H19NO4S

CAS No. 57-66-9
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms Benemid
Solubility (25°C) * In vitro DMSO 57 mg/mL (199.74 mM)
Water <1 mg/mL (<1 mM)
Ethanol 22 mg/mL (77.09 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]-

Research Area

Tech Support & FAQs

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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