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Navarixin (SCH 527123) is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively. SCH-527123 bound with high affinity to the CXCR2 receptors of mouse (K(d) = 0.20 nM), rat (K(d) = 0.20 nM), and cynomolgus monkey (K(d) = 0.08 nM) and was a potent antagonist of CXCR2-mediated chemotaxis (IC(50) approximately 3-6 nM). In contrast, SCH527123 bound to cynomolgus CXCR1 with lesser affinity (K(d) = 41 nM) and weakly inhibited cynomolgus CXCR1-mediated chemotaxis (IC(50) approximately 1000 nM). Oral treatment with SCH527123 blocked pulmonary neutrophilia (ED(50) = 1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. SCH-527123 also suppressed the pulmonary neutrophilia (ED(50) = 1.3 mg/kg), goblet cell hyperplasia (ED(50) = 0.7 mg/kg), and increase in BAL mucin content (ED(50) = <1 mg/kg) in rats after i.t. administration of vanadium pentoxide. In vivo, SCH-527123 treatment decreased tumor growth and microvessel density when compared with vehicle-treated tumors.
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Source | The University of Birmingham (2015).SCH527123, Figure 5.5. (AbMole Bioscience, Kowloon, Hong Kong) |
| Method | ||
| Cell Lines | CXCR2 and CXCR1 | |
| Concentrations | 3nM (specific to CXCR2) and 42nM (required for concurrent CXCR1 inhibition). | |
| Incubation Time | ||
| Results | Pre-incubation with the dual CXCR1/2 inhibitor (SCH527123) at both concentrations (3 nM and 42 nM) caused a significant reduction in chemokinesis in gradients of both IL-8 and GROα, but only 3 nM caused a significant reduction of chemokinesis in Sol (Figure 5.5). |
| Molecular Weight | 397.42 |
| Formula | C21H23N3O5 |
| CAS Number | 473727-83-2 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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