PKG Agonist

8-pCPT-cGMP-AM (8-(4-Chlorophenylthio)-cGMP-AM) is a highly membrane permeable prodrug of the PKG agonist 8-pCPT-cGMP, which increases the membrane permeability of cGMP and is converted to its active form by esterase hydrolysis within the cell, thereby activating PKG. 8-pCPT-cGMP-AM can be used to explore the role of cGMP signaling in neural plasticity and memory formation.

8-Br-PET-cGMP is an agonist of cGMP-dependent protein kinase type I (cGKI). 8-Br-PET-cGMP promotes the dimerization of cGKI and activates its catalytic activity by binding to the regulatory domain of cGKI. 8-Br-PET-cGMP can be used to study the role of cGMP signaling pathways in cell growth, vasodilation, and smooth muscle cell function.

PET-cGMP is a cyclic guanosine monophosphate analog and an effective selective agonist of PKG I, the EC₅₀ of PET-cGMP for PKG Iβ is 3.8 nM, while for PKG II, it's 193 nM.

Sp-8-Br-PET-cGMPS is a membrane-permeable PKG agonist and a membrane-permeable inhibitor of retinal-type cGMP-gated ion channels, as well as an activator of cGMP-dependent protein kinases I α and I β. Sp-8-Br-PET-cGMPS is resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, has no metabolic side effects, and is more lipophilic and permeable than Sp-8-pCPT-cGMPS. Sp-8-Br-PET-cGMPS can be used to study the role of cGMP signaling pathways in the nervous system.