Reparixin L-lysine salt

Biological Activity

Reparixin L-lysine salt is a potent and noncompetitive CXCR1 and CXCR2 allosteric antagonist (IC₅₀ = 1 nM for inhibition of CXCL8-induced human polymorphonuclear cell migration). Also inhibits migration of rodent neutrophils induced by CXCL1, CXCL2, CXCL8 and CINC-1. Inhibits vascular permeability and neutrophil recruitment in in vivo models of mild and severe ischemia/reperfusion injury. Also selectively depletes cancer stem cells in human breast cancer cell lines and xenograft models.

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. Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury.
   Bertini et al.
   Proc.Natl.Acad.Sci.U.S.A., 2004;101:11791
2. Repertaxin, a novel inhibitor of rat CXCR2 function, inhibits inflammatory responses that follow intestinal ischaemia and reperfusion injury.
   Souza et al.
   Br.J.Pharmacol., 2004;143:132
3. CXCR1 blockade selectively targets human breast cancer stem cells in vitro and in xenografts.
   Ginestier et al.
   J.Clin.Invest., 2010;120:485

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