CXCR2-IN-2

1838123-21-9

414.90

10 mM in DMSO

GPCR/G Protein; Immunology/Inflammation

CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in beta-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ca.730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-alpha induced CD11b expression with an IC50 of 0.04 uM.
In Vivo: CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models.