NS-2028 is a specific inhibitor of soluble guanylyl cyclase. It inhibits purified bovine lung guanylyl cyclase in a concentration dependent and irreversible manner with IC50 values of 30 and 200 nM for basal and NO-stimulated enzymes, respectively. S-nitroso-glutathione-enhanced guanylyl cyclase activity in mouse cerebellum homogenates is inhibited by NS-2028 with an IC50 value of 17 nM, making it about 4.7 fold more potent than ODQ, which has an IC50 value of 80 nM for inhibition of soluble guanylyl cyclase in the same assay. NS-2028 does not inhibit particulate guanylyl cyclase or adenylyl cyclase.
NS-2028 potent soluble guanylyl cyclase (sGC) inhibitor (Ki = 8 nM). NS-2028 blocks sGC activity in murine cerebellum induced by S-nitroso-glutathione and NMDA. NS-2028 inhibits VEGF-induced cGMP accumulation; abolishes VEGF-induced migration in postcapillary venular endothelial cells (CVEC).
Cell permeable: no', 'Primary Target
basal soluble guanylyl cyclase', 'Product does not compete with ATP.', 'Reversible: no', 'Target IC50: 30 nM for basal and 200 nM for NO-stimulated enzyme activity; 17 nM for S-nitrosoglutathione-enhanced soluble guanylyl cyclase activity in homogenates of mouse cerebellum
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].
| Animal Model: | Rabbit[2] |
| Dosage: | 1 g/L |
| Administration: | Deliver orally; 1g/L; 8 days |
| Result: | Inhibits VEGF-induced angiogenesis in vivo. |
