Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue trihydrate is a vasopressor and is often used as a dye in several medical procedures. Methylene blue trihydrate has antinociception, antimalarial, antidepressant and anxiolytic activity effects. Methylene Blue trihydrate has the potential for methemoglobinemias, neurodegenerative disorders and ifosfamide-induced encephalopathytreatment[1][2][3].
Plecanatide, an analogue of uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis[1][2][3].
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells[1].
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].
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation[1][2][3].
Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with Kd of 0.6-1.1 μM in the presence of CO.
Prepro-ANF (56-92), human is a human atrial natriuretic factor precursor. Prepro-ANF (56-92), human is also a Guanylate Cyclase activator that enhances particulate Guanylate Cyclase activity in the renal membrane and renal unit[1].
Guanylin (mouse, rat), a petide, is composed of 15 amino acids. Guanylin (mouse, rat) is an activator of intestinal guanylate cyclase. Guanylin (mouse, rat) can be used for the research of diarrhea[1].
Riociguat-d6 (BAY 632521-d6) is the deuterium labeled Riociguat. Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension[1][2].
LY83583 is a cell-permeable and competitive inhibitor of soluble guanylate cyclase (sGC) with an IC50 value of 2 µM[1].
N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect[1]-[5].
Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research[1][2].
Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects[1][2][3].
Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists[1].
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows anti-inflammatory activity in models of murine colitis[1].
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[1][2].
Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM[1].
Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure.
Ebselen oxide, the selenone analogue of Ebselen, covalently modifies diguanylate cyclase (DGC) to inhibit c-di-GMP-receptor interactions and reduces DGC activity. Ebselen oxide also inhibits alginate production (IC50=14 μM) by Pseudomonas aeruginosa. Ebselen oxide inhibits HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9 (IC50 ranging from 0.2 to 4.7 μM)[1][2][3].
BM121307 is a guanylate cyclase activator that was in phase I development for the treatment of ischaemic heart disorders. The research has been discontinued.
BAY 60-2770 is an NO-independent activator of sGC (soluble guanylyl cyclase) with EC50 of 5.4 nM; demonstrates vasodilator activity in the pulmonary and systemic vascular beds that is enhanced by ODQ and NOS inhibition.
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[1].
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research[1][2][3].
BAY 41-2272 is a soluble guanylate cyclases (sGC) activator.Target: guanylate cyclaseBAY 41-2272 is a recently introduced novel orally available agent that directly stimulates soluble guanylate cyclase (sGC) and sensitizes it to its physiological stimulator, nitric oxide. BAY 41-2272 is a promising new therapeutic agent that goes beyond current therapeutic agents. BAY 41-2272 acts as an arterial vasodilator, resulting in a reduction of MAP and pulmonary artery pressure and a decrease in SVR and renal vascular resistance. BAY 41-2272 reduces pulmonary capillary wedge pressure in the absence of a decrease in right atrial pressure. [2]
Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.
BAY-747 (BAY 1165747) is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model[1][2][3].
Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.
MGV354 is a novel potent, selective soluble Guanylate Cyclase (sGC) activator, lowers intraocular pressure (IOP) in preclinical models of glaucoma. Other Indication Phase 2 Clinical