An inhibitor of OATs and MRP1 and an agonist of TRPV2; inhibits OAT1

Probenecid – 100 g

Brand:
Cayman
CAS:
57-66-9
Storage:
-20
UN-No:
Non-Hazardous - /

Probenecid is a benzoic acid derivative that inhibits organic anion transporters (OATs) and the ATP-binding cassette transporter (ABCC1) multidrug resistance protein 1 (MRP1) and activates the transient receptor potential (TRP) channel TRPV2.{23928,23931,23929,23932,42817,42818} It inhibits OAT1, OAT3, and OAT6 (Kis = 6.3, 9.0, and 8.4 µM, respectively), as well as OAT2 (IC50 = 0.67 µM), and is selective for OATs over organic cation transporter 1 (OCT1) and OCT2 (IC50s = 1,600 and 1,700 µM, respectively).{23928,23931,23929,23932} Probenecid (7 mM) decreases Fas antibody-induced glutathione (GSH) efflux and staurosporine-induced efflux of the MRP1 substrate calcein in Jurkat cells and decreases apoptotic progression.{42818} It is an agonist of TRPV2 (EC50 = 31.9 µM).{42817} It induces nociceptive behavior in mouse models of carrageenan- or complete Freund’s adjuvant-induced inflammatory pain when administered at a dose of 20 mM in drinking water in combination with doses of carrageenan or CFA that do not provoke pain responses alone.{42817} Formulations containing probenecid have been used in the treatment of gouty arthritis.  

 

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An inhibitor of OATs and MRP1 and an agonist of TRPV2; inhibits OAT1, OAT3, and OAT6 (Kis = 6.3, 9.0, and 8.4 µM, respectively), as well as OAT2 (IC50 = 0.67 µM); selective for OATs over OCT1 and OCT2 (IC50s = 1,600 and 1,700 µM, respectively); decreases Fas antibody-induced GSH efflux and staurosporine-induced efflux of the MRP1 substrate calcein in Jurkat cells and decreases apoptotic progression at 7 mM; an agonist of TRPV2 (EC50 = 31.9 µM); induces nociceptive behavior in mouse models of carrageenan- or complete Freund’s adjuvant-induced inflammatory pain at 20 mM in drinking water in combination with doses of carrageenan or CFA that do not provoke pain responses alone

Formal name: 4-[(dipropylamino)sulfonyl]-benzoic acid

Synonyms:  NSC 18786

Molecular weight: 285.4

CAS: 57-66-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Neuroscience|Pain Research

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