cgmp

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.

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

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

Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

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.

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.

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

AP-C5 is a compound with selective inhibition of guanosine 3',5' cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), with a Pic50 value of 7.2 for cGMP, and can be used in the study of diarrheal diseases.

8-Br-PET-cGMP is an agonist of type I cyclic GMP-dependent protein kinase (cGKI), which promotes the dimerization and activation of the catalytic activity of cGKI by binding to its regulatory domain. This compound is utilized to investigate the role of the cGMP signaling pathway in cell growth, vasodilation, and smooth muscle cell functions.

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

PET-cGMP is an analogue of cyclic guanosine monophosphate and functions as a potent, selective agonist for PKGI. It exhibits an EC50 of 3.8 nM for PKGIβ and 193 nM for PKGII.

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.

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-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-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.

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].

Rp-8-pCPT-cGMPS is a competitive inhibitor of cyclic guanosine monophosphate (cGMP)-dependent protein kinase (PKG) with a Ki of 0.5 μM. This compound exhibits increased lipophilicity, allowing it to penetrate cell membranes more readily and achieve sufficient intracellular concentrations to inhibit PKG. Rp-8-pCPT-cGMPS is useful for researching the activity and function of PKG in platelets.

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.

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-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.

cGMP-dependent protein kinase (PKG) inhibitor

Sp-cGMPS serves as an activator for cGMP-dependent protein kinases (PKGs). It is frequently utilized in research related to cardiovascular diseases.