| Name | Reparixin L-lysine salt |
| Description | Reparixin L-lysine salt (Repertaxin L-lysine salt) is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor. |
| 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 5.6 nM and 80 nM for CXCR1 wt and CXCR1 Ile43Val, respectively)[1]. |
| In vivo | The pharmacokinetics and metabolism of Reparixin were investigated in rats and dogs following the intravenous administration of [14C]-Reparixin L-lysine salt. Plasma protein binding of Reparixin is >99% in both laboratory animals and humans up to 50 μg/mL, but decreases at higher concentrations. Radioactivity rapidly distributes into rat tissues, yet the volume of distribution at steady state (Vss) is low (approximately 0.15 L/kg) in both rats and dogs. Reparixin is eliminated more rapidly in rats (t1/2~0.5 h) than in dogs (t1/2~10 h)[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 99 mg/mL (230.46 mM), Sonication is recommended.
DMSO : 99 mg/mL (230.46 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.68 mM), Sonication is recommended.
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| Keywords | Repertaxin L-lysine | Repertaxin | Reparixin Llysine salt | Reparixin L-lysine | Reparixin L lysine salt | Reparixin | Inhibitor | inhibit | CXCR2 | CXCR1wt | CXCR1Ile43Val | CXCR1 | CXCR | CXC chemokine receptors |
| Inhibitors Related | AZD8309 | rac-NBI-74330 | Delmetacin | Tannic acid | Artemotil | CXCR2-IN-1 | Soquelitinib | Plerixafor octahydrochloride | Tanimilast | 3-Indoleglyoxylic acid | Nicotinamide N-oxide | CXCL-CXCR1/2-IN-1 |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
