cgmp

2'-O-MB-cGMP (2′-O-Monobutyryl-cGMP) sodium functions as an inhibitor of cyclic GMP-specific phosphodiesterases (cyclic GMP-specific phosphodiesterase), exhibiting an IC50 value of 35 µM. This compound effectively inhibits the hydrolysis of phosphodiesterases that use cAMP or cGMP as substrates in a Ca2+-dependent manner.

8-pCPT-cGMP-AM (8-(4-Chlorophenylthio)-cGMP-AM) is a highly membrane-permeable prodrug of the PKG agonist 8-pCPT-cGMP, designed to enhance membrane permeability of cGMP. It is converted into its active form within the cell via esterase hydrolysis, thus activating PKG. This compound is utilized to investigate the role of cGMP signaling in neural plasticity and memory formation.

GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD (cGMP sodium salt) , also known as cGMP, is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin. GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD activates protein kinase G (PKG) and modulates ion channel conductance, with signaling affecting diverse processes including smooth muscle relaxation and proliferation, phototransduction, and energy homeostasis.

8-Bromo-cGMP sodium is a PKG activator, a membrane-permeable analog of cGMP. 8-Bromo-cGMP sodium has pain-relieving and vasodilatory effects, significantly inhibits Ca2+ macroscopic currents, and inhibits high K+-stimulated insulin release.

Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog that preferentially activates cGMP-dependent protein kinase (PKG). It inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma thrombin and can induce peripheral analgesia by activating ATP-sensitive K+ channels.

Cys-C-cGMP serves as an autophagy tag for AUTACs (autophagy-targeting chimeras). It enhances K63-linked ubiquitination of mitochondria within HeLa cells [1].

8-Br-cGMP-AM, a derivative of 8-Br-cGMP, acts as an activator of PKG (cGMP-dependent protein kinase), inducing various biological effects such as vasodilation and platelet inhibition. This compound is utilized in the research of cardiovascular diseases.

Guanosine 2',3'-cyclic phosphate triethylamine, commonly known as 2′,3′-cGMP triethylamine, is an active compound utilizable in numerous research investigations [1].

8-Nitro-cGMP is a unique cytoprotective mediator which inhibits oxidative stress. 8-Nitro-cGMP is also a probe of the protein S-guanylation.

8-Pcpt-cGMP acts as an agonist for cyclic nucleotide-gated (CNG) channels with an EC50 of 0.5 μM and exhibits good membrane permeability. This compound is utilized in research to explore the role of CNG channels in visual and olfactory signal transduction.

cGMP-HTL, an autophagy-targeting chimera (AUTAC), consists of a HT-ligand, a linker, and a Cys-S-cGMP (autophagy tag), designed to enhance K63-linked ubiquitination of mitochondria. This novel clearance strategy features a degradation tag (guanine derivatives) and a specific warhead, facilitating targeted degradation [1].

Competitive inhibitor of cGMP-dependent protein kinase (PKG); analog of a substrate peptide corresponding to a phosphorylation site of histone H2B. Competes with synthetic substrates (Ki = 86 mM) but does not inhibit phosphorylation of intact histones by

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.

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.

Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.

Vardenafil hydrochloride trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

Sildenafil citrate (UK-92480 citrate) , a cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) Inhibitor, is used extensively for erectile dysfunction and less commonly for pulmonary hypertension.

Citronellal ((±)-Citronellal) is a monoterpene predominantly formed by the secondary metabolism of plants, producing antithrombotic, antiplatelet, and antihypertensive activities.

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

PKG Substrate acetate is a selective substrate for cGMP-dependent protein kinase (PKG).PKG Substrate is a selective substrate for protein kinase G (PKG) with a strong preference for PKG Iα (Km = 59 μM) over PKG II (Km = 305 μM).

Gisadenafil (UK-369003), a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM, prevents the degradation of cGMP.

AP-C2 is a potent small molecule guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) inhibitor with a pIC50 of 5.2 for cGKII.

T-0156 is a novel, potent and selective phosphodiesterase type 5 inhibitor that inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) with low affinity for PDE6, PDE1, PDE2, PDE3 and PDE4.

Sulmazole (AR-L 115-BS) is a small molecule Sulmazole is a small molecule cGMP-PDE inhibitor.Sulmazole is a competitive inhibitor of A1 adenosine receptors.Sulmazole has been shown to improve cardiac index, low pulmonary capillary wedge pressure, and can be used in the study of heart failure.Sulmazole is a small molecule cGMP-PDE inhibitor.

PKG inhibitor peptide TFA (82801-73-8 free base) is an inhibitor of ATP-competitive cGMP-dependent protein kinase (PKG).

Sp-8-pCPT-cGMPS is a potent agonist for cyclic guanosine monophosphate-gated (CNG) channels and serves as a lipophilic activator for PKG (types I α, I β, and II) and PKA II. It exhibits excellent cell membrane permeability and stability against phosphodiesterases. This compound is utilized in studying the role of cGMP in synaptic transmission and neural plasticity.

cGMP-dependent protein kinase (PKG) inhibitor

Sp-8-Br-PET-cGMPS is a membrane-permeable PKG activator and an inhibitor of the membrane-permeable retinal cGMP-gated ion channels (cGMP-gated ion channel). It also serves as an activator for cGMP-dependent protein kinase I α and β. Resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, Sp-8-Br-PET-cGMPS does not undergo metabolic side effects and exhibits stronger lipophilicity and permeability compared to Sp-8-pCPT-cGMPS. This compound is useful for investigating the role of the cGMP signaling pathway in the nervous system.

Sp-8-Br-cGMPS, an analogue of cGMP, acts as an agonist for cGMP gated cation channels (CNG channels) with an EC50 of 106.5 μM. While Sp-8-Br-cGMPS can induce currents, it does not stabilize channel open states as effectively as a full agonist.

Sp-8-pCPT-PET-cGMPS acts as an activator of PKG-I. It is utilized in studying the role of the NO NOS sGC PKG-I signaling pathway in cardiac differentiation.

1, 2, 3, 4, 6-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) and gallic acid from Pistacia lentiscus have antimutagenic and antioxidant activities. 2. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose (PGG) possesses potent anti-proliferative and anti-invasive effects, it also has inhibition of inducible nitric oxide synthase and cyclooxygenase-2 activity. 3. PGG may serve as a model for the development of new types of anti-diabetic and anti-metabolic syndrome therapeutics. 4. 1, 2, 3, 4, 6-Penta- O -galloyl-β- d -glucose has vasodilatory and anti-inflammatory effects, it dilates vascular smooth muscle and suppresses the vascular inflammatory process via endothelium-dependent nitric oxide (NO)/cGMP signaling. 5. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose can decrease the level of extracellular hepatitis B virus (HBV) (IC5, 1. microg/ml) in a dose-dependent manner, it also can reduce the HBsAg level by 25% at a concentration of 4 microg/ml; the gallate structure of PGG may play a critical role in the inhibition of anti-HBV activity, suggests that PGG could be a candidate for developing an anti-HBV agent. 6. 1, 2, 3, 4, 6-Penta-O-galloyl-β-D-glucose has anti-parasitic activity, displays an EC5 value of 67 μM, at least 6.6-fold more effective than the standard drug benznidazole against trypomastigote forms of T. cruzi.

MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM).

TP-10 is a selective inhibitor of PDE10A against other PDEs with IC50 of 0.8 nM.

Udenafil is an inhibitor of PDE5 .

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

MBCQ is an inhibitor of cGMP-specific phosphodiesterase PDE5.

IC87201 is a nNOS-PDZ/PSD-95-PDZ inhibitor. IC87201 showed great promise in cellular experiments and animal models of ischemic stroke and pain.

Brain natriuretic peptide-32 (BNP-32), a fragment of the proBNP cardiovascular hormone precursor, exhibits affinity for natriuretic peptide receptors in rat vascular smooth muscle cells (IC50 = 7.3 nM) and promotes cGMP accumulation within these cells (EC50 = 170 nM). Additionally, BNP-32 effectively mediates the relaxation of norepinephrine-precontracted isolated rat aortic strips (EC50 = 6.7 nM). Upon administration at a dosage of 3 µg/kg, it elevates urine and urinary electrolyte outputs and induces hypotension in rats.

Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg/ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg/ml, reduces cough induced by citric aci......

Paraxanthine-d6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine is an adenosine A1 and A2 receptor antagonist. In vivo, paraxanthine increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity, as well as inhibits motor depression induced by the adenosine A1 agonist CPA or the adenosine A2 receptor agonist CGS 21680 in rats not habituated to caffeine. It also promotes wakefulness and increases locomotor activity and core temperature in narcoleptic transgenic mice without increasing behavioral anxiety.

AP-C3 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), with a pIC50 value of 6.3, and demonstrates only weak inhibition of cGKII-dependent anion secretion [1].

AP-C1 is a potent inhibitor of cGMP-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 6.5, but only weakly inhibits cGKII-dependent anion secretion [1].

Phosphodiesterase (PDE), an enzyme capable of catalyzing the hydrolysis of the 3' ring phosphate bond in cyclic nucleotides, plays a crucial role in biochemical research and acts as a vital regulator in signal transduction processes involving the second messenger molecules cAMP and cGMP. Distinguished by their specificity to cyclic nucleotides, PDEs are categorized into different types ranging from PDE1 to PDE11, presenting potential significance in the study and treatment of various diseases [1].

PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM) .

PF04677490 is an effective PDE1 inhibitor. PF04677490 efficaciously inhibits cAMP- and cGMP-hydrolytic activity in preparations from human myocardium at concentrations selective for PDE1.

Etazolate is an inhibitor of phosphodiesterase IV that is about 8 times more active for cAMP than cGMP.