tcsc0833 SCH 563705

SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC₅₀s of 1.3 nM, 7.3 nM and K_is of 1 and 3 nM, respectively.

IC50 & Target: IC50: 1.3 nM (CXCR2), 7.3 nM (CXCR1)^[1], 5.2 nM (Mouse CXCR2)^[2]


Ki: 1 nM (CXCR2), 3 nM (CXCR1)^[1]

In Vitro: SCH 563705 (Compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC₅₀s of 1.3 nM, 7.3 nM and K_is of 1 and 3 nM, respectively. SCH 563705 shows potent inhibition against both Gro-a and IL-8 induced human neutrophil migration (chemotaxis IC₅₀ = 0.5 nM, against 30 nM of Gro-a; chemotaxis IC₅₀ = 37 nM, against 3 nM of IL-8)^[1]. SCH 563705 potently inhibits mouse CXCR2 (IC₅₀ = 5.2 nM)^[2].

In Vivo: SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys and dogs^[1]. SCH 563705 (50 mg/kg p.o) reduces blood Ly6G⁺ Ly6C⁺ neutrophil frequency and unchanged levels of Ly6GLy6Chi monocytes. SCH563705 (3-30 mg/kg p.o) treatment causes a dosedependent elevation in plasma levels of CXCL1^[2].