guanylate

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

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.

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

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.

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.

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.

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.

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.

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).

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

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.

(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).

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

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.

(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.

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

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].

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, improves cognitive performance in rats during the object location task (OLT), 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].

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.

MCUF-651 is a guanylyl cyclase A receptor positive allosteric modulators, EC50=0.45 μM.