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编 号:F251355
分子式:C9H5BrN2O3
分子量:269.05
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity. NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM. NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM. NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM). NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability.

体内研究:
NS -2028 (口服给药;1 g/L;8 天) 在 VEGF 颗粒植入后,无血管兔角膜的新血管形成显著减少。Animal Model:Rabbit
Dosage:1 g/L
Administration:Deliver orally; 1g/L; 8 days
Result:Inhibits VEGF-induced angiogenesis in vivo.

体外研究:
与在载体存在下生长的细胞相比,NS -2028 (10 μM;24 小时) 抑制 25% 的细胞数量。NS -2028 (10 μM;30 分钟) 通过抑制 p38 MAPK 激活来减弱 VEGF 诱导的 EC 迁移。
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