1. GPCR/G Protein
  2. Guanylate Cyclase
  3. NS-2028

NS-2028 

Cat. No.: HY-12379 Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

NS-2028 Chemical Structure

NS-2028 Chemical Structure

CAS No. : 204326-43-2

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Description

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].

IC50 & Target

IC50: 30 nM (soluble Guanylyl Cyclase sGC)[1]

In Vitro

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].

Cell Proliferation Assay[2]

Cell Line: HUVEC cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Decreased cell numbers in culture.

Western Blot Analysis[2]

Cell Line: HUVEC cells
Concentration: 10 μM
Incubation Time: 30 mins
Result: Attenuated VEGF-enhanced p38 phosphorylation.
In Vivo

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.
Molecular Weight

269.05

Formula

C₉H₅BrN₂O₃

CAS No.

204326-43-2

SMILES

O=C1ON=C2COC3=CC=C(Br)C=C3N21

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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NS-2028
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HY-12379
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