soluble guanylyl cyclase (sGC) inhibitor
CAS：204326-43-2
分子式：C9H5BrN2O3
分子量：269.05
纯度：98%
存储：Store at -20°C

Background:

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[1]. 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[1]. 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[1]. 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)[1]. NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability[2].

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

NS-2028 (Deliver orally; 1 g/L; 8 days) exhibits a significant reduction of new vessel formation in the avascular rabbit cornea in response to VEGF pellet implants[2].

参考文献:
[1]. Olesen SP, et al. Characterization of NS 2028 as a specific inhibitor of soluble guanylyl cyclase. Br J Pharmacol. 1998 Jan;123(2):299-309.
[2]. Morbidelli L, et al. The soluble guanylyl cyclase inhibitor NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability. Am J Physiol Regul Integr Comp Physiol. 2010 Mar;298(3):R824-32.