rp 8

cGMP-dependent protein kinase (PKG) inhibitor

Rp-8-bromo-Cyclic AMPS (Rp-8-bromo-cAMPS) is a cell-permeable cAMP analog that combines an exocyclic sulfur substitution in the equatorial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP. It acts as an antagonist of cAMP-dependent protein kinases (PKAs) and is resistant to hydrolysis by cyclic nucleotide phosphodiesterases. Rp-8-bromo-cAMPS more effectively antagonizes cAMP-dependent activation of purified PKA type I from rabbit muscle than PKA type II from bovine heart.

Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]

Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase.

Rp-8-Br-cAMPS acts as an inhibitor of PKA. By binding to the cAMP binding sites on the regulatory subunits, Rp-8-Br-cAMPS prevents the dissociation and activation of PKA. Additionally, it enhances immune function in mouse models of retroviral infection.

Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMPS) sodium salt acts as an effective activator of Ca2+-ATPase. Additionally, it serves as an agonist for rod CNG channels and an inhibitor of PKG. Rp-8-Br-cGMPS sodium salt mediates the reduction of cytoplasmic Ca2+ by activating the Ca2+-ATPase enzyme, consequently removing Ca2+ from the cell.

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.

CGRP 8-37 (rat) is a CGRP receptor antagonist, a CGRP fragment with potential anti-injury effects that induces arterial relaxation.

RP-72540 is a cholecystokinin B receptor antagonist. RP 72540 showed selectivity factors in express of 200 for CCKA versus CCKB receptors and also had high affinity for gastrin binding sites in the stomach. Administration of RP-72540 resulted in a dose-de