Reparixin L-lysine salt

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Cat.No. 6957 - Reparixin L-lysine salt | C14H21NO3S.C6H14N2O2 | CAS No. 266359-93-7
Description: Potent CXCR1 and CXCR2 allosteric antagonist
Alternative Names: Repertaxin L-lysine salt
Chemical Name:R)-α-Methyl-4-(2-methylpropyl)-N-(methylsulfonyl)benzeneacetamide L-Lysine salt
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

M. Wt 429.58
Formula C14H21NO3S.C6H14N2O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 266359-93-7
PubChem ID 9932389
InChI Key JEJFWWFZAQBZMJ-GVKMLHTLSA-N
Smiles NCCCC[C@H](N)C(O)=O.CC(C)CC1=CC=C(C=C1)[C@@H](C)C(=O)N[S](C)(=O)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.48 50
water 2.15 5 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 429.58. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.66 mL 23.28 mL 46.56 mL
2.5 mM 0.93 mL 4.66 mL 9.31 mL
5 mM 0.47 mL 2.33 mL 4.66 mL
25 mM 0.09 mL 0.47 mL 0.93 mL

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References

References are publications that support the biological activity of the product.

Bertini et al (2004) Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc.Natl.Acad.Sci.U.S.A. 101 11791 PMID: 15282370

Souza et al (2004) Repertaxin, a novel inhibitor of rat CXCR2 function, inhibits inflammatory responses that follow intestinal ischaemia and reperfusion injury. Br.J.Pharmacol. 143 132 PMID: 15302676

Ginestier et al (2010) CXCR1 blockade selectively targets human breast cancer stem cells in vitro and in xenografts. J.Clin.Invest. 120 485 PMID: 20051626


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Citations for Reparixin L-lysine salt

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