guanylate cyclase-in-1

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

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

KMUP-1 is a xanthine derivative known for its vasodilatory properties. It functions as a phosphodiesterase (PDE) inhibitor and an activator of soluble guanylate cyclase (sGC), engaging the NO/sGC/cyclic guanosine monophosphate pathway. Additionally, KMUP-1 can open K+ channels and has the potential to alleviate ischemia-induced cardiac myocyte apoptosis (apoptosis). This compound is useful in cardiovascular and anti-inflammatory research.

sGC stimulator 1 is a carbonyl sulfide (COS)/H2S donor hybrid soluble guanylate cyclase (sGC) stimulator with an EC50 of 496 nM. It demonstrates significant H2S release properties and reduces fibrosis in cardiac fibroblasts treated with TGF-β1 by increasing H2S levels. sGC stimulator 1 exerts antifibrotic effects by activating sGC and elevating H2S concentrations. This compound is applicable for heart failure (HF) research[1].

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].

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]

Nicorandil-D4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil (T0075) 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 (T0075) 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 (T0075) 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.

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].

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].

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 (mouse, rat), a 15-amino-acid peptide, activates intestinal guanylate cyclase and is employed in diarrhea research [1].

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].

C-Type Natriuretic Peptide (1-53), from porcine, rat, and mouse sources, serves as an activator of particulate guanylate cyclase B (pGC-B), prominently found in endothelial cells, kidneys, and the heart. This peptide efficiently mediates a potent anti-fibrotic effect in human cardiac and renal fibroblasts through the production of the second messenger cGMP.