产品描述
SCH 563705 is an effective and orally available CXCR2 and CXCR1 antagonist (IC50s: 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively).
体外活性
SCH 563705 potently inhibits mouse CXCR2 (IC50 = 5.2 nM). SCH 563705 displays 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][2].
体内活性
SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys, and dogs. SCH563705 (3-30 mg/kg p.o) treatment causes a dose-dependent elevation in plasma levels of CXCL1. SCH 563705 (50 mg/kg p.o) decreases blood Ly6G+ Ly6C+ neutrophil frequency and unchanged levels of Ly6GLy6Chi monocytes [1][2].
Cas No.
473728-58-4
分子式
C23H27N3O5
分子量
425.48
储存和溶解度
DMSO:30 mg/mL (70.51 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years