guanylate

Guanylate cyclase-IN-1 (Example 46) is a specific inhibitor of guanylate cyclase, employed in research related to cardiovascular diseases.

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.

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

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

Cinaciguat (BAY 58-2667) (BAY 58-2667) is the first of a new class of soluble guanylate cyclase (sGC) activators in Clinicalal development for acute decompensated heart failure.

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.

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).

Prepro-Atrial Natriuretic Factor (26-55) (human) is a polypeptide that elevates cyclic GMP levels in the renal cortex and medulla and enhances renal guanylate cyclase activity [1].

(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).

Methylene Blue (Basic Blue 9) hydrate functions as an inhibitor of guanylyl cyclase (sGC), monoamine oxidase A (MAO-A), and NO synthase (NOS). This compound, known for its vasopressor activity, is widely utilized as a dye in various medical procedures. It operates via the nitric oxide synthase/guanylate cyclase signaling pathway to diminish prepulse inhibition and possesses the capacity to cross the blood-brain barrier. Methylene Blue hydrate acts as a REDOX cycling compound and inhibits Tau protein aggregation. Moreover, it is effective in reducing cerebral edema, damping microglial activation, and alleviating neuroinflammation, demonstrating its multifaceted therapeutic potential [1] [2] [3].

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.

MM 419447 is a guanylate cyclase-C agonist, and it is a metabolite of linaclotide. This compound, MM 419447, shows promise in the field of irritable bowel syndrome with constipation (IBS-C) research.

Indusatumab (5F9 Monoclonal antibody) is an anti-human GUCY2C (Guanylate cyclase 2C) monoclonal antibody that can be used to synthesize antibody-drug conjugate.

Uroguanylin-15 (Rat) is a bioactive natriuretic peptide hormone that modulates sodium excretion in response to high NaCl intake by activating guanylate cyclase signaling pathways in the intestine and kidney. Initially isolated from rat urine and duodenum, it shares functional similarities with guanylin but has not been detected in rat colon extracts.

2'-Deoxyguanosine 5'-monophosphate (dGMP) is used as a substrate of guanylate kinases to generate dGDP, which in turn is phosphorylated to dGTP, a nucleotide precursor used in DNA synthesis. In addition, dGMP can be efficiently phosphorylated by the type I thymidylate kinase of the malarial agent P. falciparum. In humans, deficiency of mitochondrial deoxyguanosine kinase, which synthesizes dGMP from ATP and deoxyguanosine, contributes to mitochondrial DNA depletion syndrome.

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.

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

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.

BAY-747 (BAY 1165747) is an orally administered, brain-penetrant compound that stimulates soluble guanylate cyclase (sGC). It effectively counteracts memory impairments induced by L-NAME and improves cognitive performance in rats during the object location task (OLT). Additionally, BAY-747 reduces blood pressure in conscious normotensive and spontaneously hypertensive rats (SHR) and enhances skeletal muscle function in the mdx/mTRG2 mouse model of Duchenne muscular dystrophy (DMD) [1] [2] [3].

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

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.

Riociguat-13C-d6 is the 13C and deuterated compound of Riociguat. Riociguat has a CAS number of 625115-55-1. Riociguat is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.

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.

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

BAY 41-8543 is a nitric oxide (NO)-independent stimulator of soluble guanylyl cyclase (sGC).

Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg/kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.

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

Dolcanatide, an orally active guanylate cyclase-C (GC-C) agonist, exhibits laxative, anti-nociceptive, and anti-inflammatory properties. It is utilized in research concerning inflammatory bowel disease [1] [2].

Guanylin (human) TFA is a 15-amino acid peptide that serves as an endogenous activator of intestinal guanylate cyclase. This compound is primarily located in the gastrointestinal tract, where it regulates electrolyte and water transport in the intestinal and renal epithelia through a mechanism dependent on cyclic GMP. [1][2]

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.

Indusatumab vedotin (MLN-0264; AKT-264) is an antibody-drug conjugate (ADC) that combines a human anti-guanylate cyclase C (GCC) antibody with the microtubule-disruptor monomethyl auristatin E, demonstrating anti-proliferative effects on pancreatic cancer cell lines by arresting the cell cycle at the G2/M phase and inducing apoptosis [1].

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].

Guanylin (mouse, rat), a peptide consisting of 15 amino acids, acts as an activator of intestinal guanylate cyclase and is utilized in diarrhea research [1].

Zagociguat is a soluble guanylate cyclase stimulator that enhances nitric oxide (NO) signaling, resulting in increased production of cyclic guanosine monophosphate. This compound shows promise for investigating non-central nervous system (CNS) disorders.

Mosliciguat is a guanylate cyclase activator.

BAY 41-2272 is a direct and NO-independent soluble guanylate cyclase (sGC) stimulator.

SGC agonist 1 is a potent soluble guanylate cyclase (SGC) agonist. SGC agonist 1 is able to increase solubility and has high cell permeability.

Vericiguat-d3 is a deuterated compound of Vericiguat. Vericiguat has a CAS number of 1350653-20-1. Vericiguat is a potent and orally available guanylate cyclase stimulator.

Ataciguat (HMR-1766) (HMR-1766) is a potent and specific soluble guanylate cyclase (sGC) activator.

NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor (IC50: 30 nM and 200 nM for basal and NO-stimulated enzyme activity). It is commonly used in the research of nitric oxide signaling pathways. NS-2028 inhibits soluble Guanylyl Cyclase

SGC agonist 2 is a potent soluble guanylate cyclase (SGC) agonist. SGC agonist 2 has potential for cardiovascular disease (heart failure, angina, pulmonary hypertension, myocardial infarction) and fibrotic disease (renal fibrosis, systemic sclerosis).

CFM 1571 hydrochloride is a chemical compound that acts as a stimulator of the nitric oxide receptor known as soluble guanylate cyclase (sGC). It demonstrates an EC50 value of 5.49 μM and an IC50 value of 2.84 μM. Soluble guanylate cyclase is an important signal-transduction enzyme that is activated by nitric oxide. The compound CFM 1571 hydrochloride shows potential for use in cardiovascular and other disease research [1] [2].

Plecanatide acetate is an analogue of Uroguanylin. It is an orally active guanylate cyclase-C (GC-C) receptor agonist.

Prepro-ANF (56-92), human, a precursor to the human atrial natriuretic factor, serves as an activator of guanylate cyclase, specifically enhancing particulate guanylate cyclase activity within the renal membrane and unit [1].

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.

Vardenafil-d5 is a deuterated compound of Vardenafil. Vardenafil has a CAS number of 224785-90-4. Vardenafil (Levitra) 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.

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