NS-2028 是一种高度选择性的可溶性鸟苷酸环化酶抑制剂。它抑制 3-吗啉代-sydnonimine 在人培养的脐静脉内皮细胞中形成环状GMP，IC50为30mM。它抑制小鼠小脑匀浆和神经元 NO 合酶中的可溶性鸟苷酸环化酶活性，IC50分别为 17 和 20 mM。它可降低血管内皮生长因子诱导的血管生成和通透性。

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.

NS-2028 (10 μM; 30 mins) decreases VEGF-induced EC migration by inhibiting p38 MAPK activation. NS-2028 (10 μM; 24 hours) inhibits 25% cell number in comparation with those grown in the presence of a vehicle[2].

In the avascular rabbit cornea, NS-2028 (p.o; 1 g/L; 8 days) displays an obvious reduction of new vessel formation in response to VEGF pellet implants[2].

204326-43-2

C9H5BrN2O3

269.05

DMSO:250 mg/mL (929.20 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years