Probenecid

Biological Activity

Probenecid is an inhibitor of multidrug resistance-associated proteins (MRP). Probenicid inhibits OAT3, organic acid transport in the kidney and other organs and exhibits inhibitory activity against pannexin 1 channels (IC₅₀ ~ 150 μM). Probenecid potently inhibits SARS-CoV-2 replication in NHBE and Vero E6 cells (IC₅₀ = 1.3 nM and 750 nM, respectively) and reduces lung virus titers in vivo. Probenicid also inhibits influenza A virus replication in vitro and in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. C3a modulates IL-1beta secretion in human monocytes by regulating ATP efflux and subsequent NLRP3 inflammasome activation.
   Asgari E, Le Friec G, Yamamoto H, Perucha E, Sacks S, Kohl J, Cook H, Kemper C
   Blood, 2013;122(20):3473-81.
2. Mitochondrial ROS induced by chronic ethanol exposure promote hyper-activation of the NLRP3 inflammasome
   LR Hoyt, MJ Randall, JL Ather, DP DePuccio, CC Landry, X Qian, YM Janssen-He, A van der Vl, AE Dixon, E Amiel, ME Poynter
   Redox Biol, 2017;12(0):883-896.
3. Glutathione export during apoptosis requires functional multidrug resistance-associated proteins.
   Hammond et al.
   J.Biol.Chem., 2007;282:14337
4. Probenecid, a gout remedy, inhibits pannexin 1 channels.
   Silverman et al.
   Am.J.Physiol.Cell Physiol., 2008;295:C761
5. Function and expression of ATP-binding cassette transporters in cultured human Y79 retinoblastoma cells.
   Ishikawa et al.
   Biol.Pharm.Bull., 2010;33:504
6. Clinical pharmacokinetics of probe.
   Cunningham et al.
   Clin.Pharmacokinet., 1981;6:135
7. Targeting organic anion transporter 3 with probenecid as a novel anti-influenza a virus strategy.
   Perwitasai et al.
   Antimicrob.Agents Chemother., 2013;57:475

Product Datasheets