A novel potent soluble guanylate cyclase (sGC) activator.

Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.

BAY 41-2272 is a soluble guanylate cyclase agonist, activates human mononuclear phagocytes

NS 2028 is a specific inhibitor of soluble guanylyl cyclase.

Praliciguat (IW-1973, IW1973) is a potent, orally available sGC stimulator that concentration-dependently increases the production of cGMP with EC50 of 267 nM.

YC-1(Lificiguat) is a soluble guanylyl cyclase(sGC) activator; binds to the heme-containing domain of the β subunit with Kd value of 0.6-1.1 μM in the presence of CO.

Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.

Guanylin(human), a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.

Guanylin(human) TFA, a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) TFA is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.

Guanylate cyclase-IN-1 (Example 46) is a guanylate cyclase inhibitor that can be used for cardiovascular diseases research.

MM 419447, a linaclotide metabolite, is a guanylate cyclase-C agonist. MM 419447 has the potential for the research of the irritable bowel syndrome with constipation (IBS-C).

Mosliciguat is a guanylate cyclase activator.

Zagociguat is the stimulator of soluble guanylate cyclase. Zagociguat increases nitric oxide (NO) signaling leading to an increase in cyclic guanosine monophosphate production. Zagociguat has the potential for the research of noncentral nervous system (CNS) disorders.

CFM 1571 hydrochloride is the stimulator of the nitric oxide receptor, soluble guanylate cyclase (sGC) with an EC50 and IC50 of 5.49 μM and 2.84 μM, respectively. Soluble guanylate cyclase (sGC) is a key signal-transduction enzyme activated by nitric oxide (NO). CFM 1571 (hydrochloride) (compound 32) has the potential for the research of cardiovascular and other diseases.

A potent, selective soluble guanylate cyclase (sGC) stimulator that increases sGC activity (cGMP formation) with EC50s of 27 and 25 nM for rat and human sGC, respectively; displays 23-fold selectivity for sGC over OATP1B1 and >197-fold selectivity over a panel of 38 proteins; increases P-VASP levels in rat aortic smooth muscle cells with EC50 of 12.7 nM; attenuates the development of cardiac hypertrophy in a blood pressure-independent fashion.

BAY-747 (BAY747) is a novel potent, selective, brain-penetrant soluble guanylate cyclase (sGC) stimulator.Oral administration of BAY-747 to male Wistar rats enhanced memory acquisition in the object location task (OLT), reversed L-NAME induced memory impairments in the OLT.BAY-747 enhanced hippocampal GluA1-containing AMPA receptor (AMPAR) trafficking in a chemical LTP model for memory acquisition using acute mouse hippocampal slices in ex vivo.

C-type natriuretic peptide (CNP, pGC-B activator) is the native particulate guanylyl cyclase B receptor (pGC-B) activator.CNP induces anti-remodeling actions in the heart and kidney through the generation of the second messenger cGMP.CNP selectively activates pGC-B and generates cGMP in vitro.CNP is abundantly expressed in the endothelium and kidneys as well as the heart, but to lesser extent than trial natriuretic peptide (ANP) and b-type natriuretic peptide (BNP).CNP is produced as a prohormone that is cleaved intracellularly by the enzyme, furin, to yield a 53-AA intermediate form (C53).

Human C53 peptide (C53, pGC-B activator C53) is a novel potent, selective particulate guanylyl cyclase B (pGC-B) activator, activates pGC-B/cGMP signaling pathway, and enhances cGMP generating actions.C53 is highly resistant to NEP degradation and has less interaction with NPRC compared to CNP in vitro.C53 activates the protective pGC-B/cGMP signaling pathway and possesses enhanced cGMP generating actions.C53 inhibits fibroblast proliferation chronically and suppresses the differentiation of fibroblasts to myofibroblasts.

MCUF-651 (MCUF651) is a small molecule guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM), potentiate ANP-mediated cGMP with EC50 of 0.45 uM (Emax=82%) in HEK293 GC-A cells.MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro.MCUF-651 binds to GC-A (Kd=397 nM) and selectively enhances the binding of ANP to GC-A ( MCUF-651+ANP, Kd=0.06 nM).MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP to generate GC-A-mediated cGMP ex vivo.

Rat C53 peptide (C53, pGC-B activator C53) is a novel potent, selective particulate guanylyl cyclase B (pGC-B) activator, activates pGC-B/cGMP signaling pathway, and enhances cGMP generating actions.C53 is highly resistant to NEP degradation and has less interaction with NPRC compared to CNP in vitro.C53 activates the protective pGC-B/cGMP signaling pathway and possesses enhanced cGMP generating actions.C53 inhibits fibroblast proliferation chronically and suppresses the differentiation of fibroblasts to myofibroblasts.