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Reparixin L-lysine salt Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5753810

Reparixin L-lysine salt is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor. More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Reparixin L-lysine salt, Inhibitor
Full Product Name
Reparixin L-lysine salt
Product Synonym Names
Repertaxin L-lysine salt
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
429.57
Solubility
H2O: 100mg/mL (232.79mM) Need ultrasonic
DMSO: 100mg/mL (232.79mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C20H35N3O5S
SMILES
N[C@@H](CCCCN)C(O)=O.CS(=O)(NC([C@@H](C1=CC=C(CC(C)C)C=C1)C)=O)=O
CAS Number
266359-93-7
Target & IC50
CXCR1wt: ic50 5.6nM (in L1.2 cells)
CXCR1Ile43Val: ic50 80nM (in L1.2 cells)
CXCR1: ic50 1nM (in cells)
CXCR2: ic50 100nM (in cells)
In Vitro
Reparixin is a potent CXCL8-induced inhibitor biological activities on human PMNs, with a marked selectivity (around 400-fold) for CXCR1, as shown in specific experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs.Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2[2]. The efficacy of Reparixin is significantly lower in L1.2 cells expressing Ile43Val CXCR1 mutant (IC50 values of 5.6nM and 80nM for CXCR1 wt and CXCR1 Ile43Val, respectively)[1].

Product References and Citations for Reparixin L-lysine salt, inhibitor

Moriconi A, et al. Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2. J Med Chem. 2007 Aug 23;50(17):3984-4002.
Moriconi A, et al. Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2. J Med Chem. 2007 Aug 23;50(17):3984-4002.
Bertini R, et al. Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2non-competitive allosteric inhibitor. Br J Pharmacol. 2012 Jan;165(2):436-54.
Bertini R, et al. Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2non-competitive allosteric inhibitor. Br J Pharmacol. 2012 Jan;165(2):436-54.
Midgley I, et al. Species differences in the pharmacokinetics and metabolism of reparixin in rat and dog. Xenobiotica. 2006 May;36(5):419-40
Midgley I, et al. Species differences in the pharmacokinetics and metabolism of reparixin in rat and dog. Xenobiotica. 2006 May;36(5):419-40
Catrina, Anca, et al. METHODS AND COMPOUNDS FOR THE treatment,OF BONE LOSS AND/OR PAIN. US 20170105971 A1.
Catrina, Anca, et al. METHODS AND COMPOUNDS FOR THE treatment,OF BONE LOSS AND/OR PAIN. US 20170105971 A1.
Bertini R, et al. Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6.
Bertini R, et al. Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6.

Other Notes

Small volumes of Reparixin L-lysine salt, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

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MBS5753810 is an inhibitor targeting Reparixin L-lysine salt.
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