Probenecid - Moligand™, 10mM in DMSO , Solute carrier family 22 member 11 inhibitor, CAS No.57-66-9, Solute carrier family 22 member 11 inhibitor

CAS: 57-66-9 Cat. No.: P408015 Molecular Weight: 285.36 EC Number: 200-344-3

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-(Di-n-propylaminosulfonyl)benzoic acid | 4-(Di-n-propylsulfamoyl)benzoic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Probenecid 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.
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. 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. 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. 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.

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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

4-(Di-n-propylaminosulfonyl)benzoic acid | 4-(Di-n-propylsulfamoyl)benzoic acid

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ACTIVATOR, ANTAGONIST, INHIBITOR

Mechanism of action

Solute carrier family 22 member 11 inhibitor

Product Properties

• ALogP: 3.2

Names and Identifiers

• Isomeric SMILES: CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(=O)O
• WGK Germany: 3
• RTECS: DG9400000
• UN Number: 3249
• Packing Group: II
• Molecular Weight: 285.36
• Reaxy-Rn: 2815775
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2815775&ln=

Associated Targets(Human)

SLC22A6 Tclin Solute carrier family 22 member 6 (1 Activities)

Discover Target: SLC22A6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRPV2 Tchem Transient receptor potential cation channel subfamily V member 2 (1 Activities)

Discover Target: TRPV2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA2 Tclin Carbonic anhydrase 2 (3 Activities)

Discover Target: CA2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA9 Tclin Carbonic anhydrase 9 (3 Activities)

Discover Target: CA9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 198-199°C

References

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