NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor (IC50: 30 nM and 200 nM for basal and NO-stimulated enzyme activity). It is commonly used in the research of nitric oxide signaling pathways. NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase (IC50: 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 (IC50: 30 nM). NS-2028 inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM). NS-2028 decreases vascular endothelial growth factor-induced angiogenesis and permeability.

sGC:30 nM

NS-2028 (10 μM; 30分钟) 通过抑制p38 MAPK的激活，降低VEGF诱导的EC迁移。NS-2028 (10 μM; 24小时) 与那些在载体存在下生长的细胞相比，抑制了25%的细胞数量[2]。

在无血管的兔角膜中，NS-2028（p.o; 1 g/L; 8天）对VEGF颗粒植入的新血管形成有明显的抑制作用[2]。