SCH 563705CAS号: 473728-58-4分子式: C23H27N3O5分子量: 425.48描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
SCH563705, SCH-563705
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可溶性/溶解性 |
10 mM in DMSO
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生物活性 | |
靶点 |
CXCR
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In vitro(体外研究) |
SCH 563705 (Compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis 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). SCH 563705 potently inhibits mouse CXCR2 (IC50 = 5.2 nM).
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In vivo(体内研究) |
SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys and dogs. 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.
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分子结构图