guanylate

Guanylate cyclase-IN-1 (Example 46) is a specific guanylate cyclase inhibitor used in cardiovascular disease research.

Glutaminyl Cyclase Inhibitor 1, a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM, can be utilized for studying neurological disorders.

LY83583 is a soluble guanylate cyclase competitive inhibitor with IC50 of 2 µM.

Sinitrodil (ITF-296) is a guanylate cyclase stimulant that may be used in the treatment of myocardial ischemia and angina pectoris.

Methylene Blue trihydrate (Basic blue 9) is a compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene Blue trihydrate is used as a bacteriologic stain and as an indicator. It inhibits soluble guanylyl cyclase and has been used to treat cyanide poisoning and to lower levels of methemoglobin. It also inhibits tau filament formation (IC50: 1.9μM).

Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Riociguat (BAY 632521) is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.

Nitroprusside disodium dihydrate (Sodium Nitroprusside Dihydrate) is a potent vasodilator working through releasing NO spontaneously in blood.

Nelociguat (BAY60-4552)(BAY60-4552) is a soluble guanylate cyclase stimulator (sGC stimulator). Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway.

Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).

NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor (IC50: 30 nM and 200 nM for basal and NO-stimulated enzyme activity) commonly used in nitric oxide signaling pathway research. It inhibits sGC activity in mouse cerebellum homogenates and neuronal NO synthase (IC50: 17 nM and 20 nM), inhibits 3-morpholino-sydnonimine (SIN-1)-elicited cyclic GMP formation in human cultured umbilical vein endothelial cells (IC50: 30 nM), and completely inhibits NO-dependent relaxant responses in non-vascular smooth muscle (1 μM). NS-2028 also decreases vascular endothelial growth factor-induced angiogenesis and permeability.

BI 703704, a soluble guanylate cyclase (sGC) activator, inhibits the progression of diabetic nephropathy in the ZSF1 rat [1].

(4-Acetamidocyclohexyl) nitrate (BM121307) is an activator of guanylate cyclase.

Linaclotide, developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, is a potent and selective guanylate cyclase C agonist.

Linaclotide acetate is used as an oral guanylate cyclase C agonist linaclotide; 14 amino acid peptide for the potential treatment of constipation-predominant irritable bowel syndrome and chronic idiopathic constipation.

Plecanatide acetate is a agonist of guanylate cyclase-C (GC-C) receptor( EC50 of 190 nM in T84 cells), and shows anti-inflammatory activity in models of murine colitis.

(Rac)-MGV354 (MGV354) is the racemate of MGV354. MGV354 is a soluble activator of guanylate cyclase (sGC)(EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively).

MGV354 is a soluble activator of guanylate cyclase(sGC) with EC 50 s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively [1] [2].

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

Praliciguat (IW-1973) stimulates sGC in HEK-293 cells (EC50: 197 nM). Praliciguat is an effective and orally active soluble guanylate cyclase stimulator. It also enhances NO signaling and acts as a vasodilator.

Runcaciguat is a soluble guanylate cyclase stimulator. Runcaciguat combines with selective partial adenosine A1 receptor agonists and can be used in studies about cardiovascular and renal diseases.

Vericiguat (BAY1021189) is a potent and orally available guanylate cyclase stimulator.

ODQ is an effective and selective soluble guanylyl cyclase (sGC) inhibitor.