NS-2028 is a potent soluble guanylyl cyclase (sGC) inhibitor with Ki of 8 nM. NS-2028 inhibits sGC activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 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].

Plecanatide is an oral guanylate cyclase C agonist acting locally in the gastrointestinal tract, it is approved in January 2017 by the FDA for the treatment of chronic idiopathic constipation (CIC).

ODQ is a selective and irreversible inhibitor of nitric oxide-sensitive guanylyl cyclase.

Cinaciguat is the first of a class of soluble guanylate cyclase (sGC) activators in clinical development for acute decompensated heart failure.

Linaclotide is a 14-amino acid peptide indicated for the treatment of adults with CC and IBS-C and an agonist of guanylate cyclase C

Vericiguat targets soluble guanylate cyclase (sGC) and is used for treating heart failure.

BAY 41-2272 is an activator of guanylate cyclases (sGC).

Ataciguat is a potent guanylate cyclase activator potentially for the treatment of aortic valve stenosis.

Riociguat acts as stimulator of soluble guanylate cyclase (sGC) that is used to treat ipulmonary hypertension.

Lificiguat is an acivator of guanylyl cyclase (sGC) and can bind to the heme-containing domain of the β subunit with Kd of 0.6 μM - 1.1 μM.