Reparixin L-lysine salt, Inhibitor

Reparixin L-lysine salt

Cat. Num. AAA5753810

• Purity: 98.00%
• Synonyms: Reparixin L-lysine salt; Repertaxin L-lysine salt; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• 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].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Reparixin L-lysine salt, inhibitor

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

Product Categories/Family for Reparixin L-lysine salt, inhibitor

Autophagy; CXCR; GPCR/G Protein; Immunology/Inflammation

References

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.