SCH-527123，5MG，SML4039-5MG，Sigma

Biochem/physiol Actions

Orally active, high-affinity, potent and selective allosteric CXCR2 antagonist.

SCH-527123 is an orally active, high-affinity, potent and selective allosteric CXCR2 antagonist (IC50 = 2.6 nM) with much reduced CXCR1 potency (IC50 = 36 nM) and little activity against a large panel of enzymes, channels, and GPCRs (IC50 >10 µM). SCH-527123 blocks CXCL8- and CXCL1-induced human neutrophil (hPMN) chemotaxis in cultures (IC50 = 16 & <1 nM, respectively) and pulmonary neutrophilia in vivo (ED50 = 1.2 mg/kg mouse, 1.8 mg/kg rat p.o.) following intranasal LPS administration.