All AbMole products are for research use only, cannot be used for human consumption.
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.
.sch527123, figure 5.5..jpg) |
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 |
| Related CXCR Products |
|---|
| Plerixafor (AMD3100)
Plerixafor (AMD3100) is a CXCR4 chemokine receptor antagonist. |
| WZ 811
WZ811 is a highly competitive CXCR4 antagonist with oral activity. WZ811 effectively inhibited CXCR4/SDF-1 (also known as CXCL12) -mediated regulation of cAMP level (EC50=1.2 nM) and SDF-1-induced matrix glue invasion (EC50=5.2 nM) in cells. |
| AMD3465 hexahydrobromide (AMD3465 )
AMD3465 hexahydrobromide（AMD3465 ) is an effective CXCR4 antagonist that inhibits 12G5 mAb in SupT1 cells. The IC50 values of CXCL12AF647 and CXCR4 were 0.75 nM and 18 nM, respectively. AMD 3465 also effectively inhibited X4 HIV replication (IC50, 1-10 nM), but not R5 HIV replication. |
| Plerixafor 8HCl
Plerixafor 8HCl (AMD3100 8HCl) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively. |
| SB225002
SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM and >150-fold selectivity over CXCR1 and four other 7-TMRs. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
