产品
编 号：F087141
分子式：C19H16BFN2O3S
分子量：382.22
分子式：C19H16BFN2O3S
分子量：382.22
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1240494-13-6
产品详情
生物活性：
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model.
体内研究：
SX-517 (化合物7) (0.2 mg/kg; 静脉注射; 单剂量) 显著抑制体内小鼠模型炎症。Animal Model:Male CD1 SWISS mice with an air-pouch on the backs (10-15 week old)
Dosage:0.02 mg/kg, 0.2 mg/kg
Administration:Intravenous injection; single dose
Result:Significant reduction in cell count in the pouches of treated animals compared to the positive control cohort.
体外研究：
SX-517 (化合物7) (0.1 nM-0.1 mM; 60 min) 有效抑制 10 nM CXCL8 诱导的 [35S]GTPγS 结合，IC50 为 60 nM。Sx-517 (10 μM; 60 min) 对 HEK293 细胞中 CXCR2 细胞表面表达有抑制作用。Sx-517 (10 μM; 0-30分钟) 阻断 HEK293 细胞中 CXCR2 介导的 ERK1/2 磷酸化。
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model.
体内研究：
SX-517 (化合物7) (0.2 mg/kg; 静脉注射; 单剂量) 显著抑制体内小鼠模型炎症。Animal Model:Male CD1 SWISS mice with an air-pouch on the backs (10-15 week old)
Dosage:0.02 mg/kg, 0.2 mg/kg
Administration:Intravenous injection; single dose
Result:Significant reduction in cell count in the pouches of treated animals compared to the positive control cohort.
体外研究：
SX-517 (化合物7) (0.1 nM-0.1 mM; 60 min) 有效抑制 10 nM CXCL8 诱导的 [35S]GTPγS 结合，IC50 为 60 nM。Sx-517 (10 μM; 60 min) 对 HEK293 细胞中 CXCR2 细胞表面表达有抑制作用。Sx-517 (10 μM; 0-30分钟) 阻断 HEK293 细胞中 CXCR2 介导的 ERK1/2 磷酸化。
产品资料
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