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CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-fold selectivity over CXCR1 and greater than 1900-fold selectivity over all other chemokine receptors. Furthermore, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood, displaying an IC50 of 0.04 μM[1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | 1.330 € | 8-10 weeks | |
50 mg | 1.729 € | 8-10 weeks | |
100 mg | 2.679 € | 8-10 weeks |
Description | CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-fold selectivity over CXCR1 and greater than 1900-fold selectivity over all other chemokine receptors. Furthermore, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood, displaying an IC50 of 0.04 μM[1]. |
Targets&IC50 | CXCR1:3.8 μM (IC50), CXCR2:5.2 nM (IC50) |
In vivo | CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in rat and mouse air pouch models in vivo[1]. |
Alias | CXCR2-IN-2 |
Molecular Weight | 414.9 |
Formula | C18H23ClN2O5S |
Cas No. | 1838123-21-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 240 mg/mL (578.45 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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