SCH 563705 is a potent and orally availableCXCR2andCXCR1antagonist, withIC₅₀s of 1.3 nM, 7.3 nM andK_is of 1 and 3 nM, respectively.

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].

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].

425.48

Solid

C₂₃H₂₇N₃O₅

473728-58-4

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 30 mg/mL(70.51 mM)

*"≥" means soluble, but saturation unknown.

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