Biological Activity
ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC50 of 2.3 μM.
In Vitro
ST034307 reveals selective inhibition of AC1 and potentiates AC8 activity to a nonsignificant small extent. ST034307 potentiates phorbol 12-myristate 13-acetate (PMA)-stimulated cAMP production by AC2. ST034307 significantly inhibits the forskolin- or isoproterenol-stimulated AC1 activity in HEK cells stably expressing AC1. In contrast, ST034307 has no significant effects in the wild-type HEK cells. ST034307 significantly inhibits the Ca2+/calmodulin-stimulated cAMP accumulation in the hippocampal homogenates. ST034307 dose-dependently inhibits both the development and the maintenance of MOR-mediated sensitization of AC1[1].
In Vivo
ST034307 (0.25 μg) causes a significant relief of CFA-induced inflammatory pain in mice. ST034307 exhibits an estimated median effective dose (E50) value for analgesia of 0.28 μg in the mouse pain model[1].
Target
IC50: 2.3 μM (AC1)[1]
Cell Assay
Cell viability assays are conducted with HEK-AC1 cells following plating and compound incubation protocols identical to the procedures described in “cAMP accumulation in cells.” Cell viability is measured as a percentage of vehicle using 2% Triton X-100 as a control. The CellTiter-Glo Luminescent Cell Viability Assay kit from Promega is used to assess cell viability according to the manufacturer’s instructions. Luminescence counts are measured using Synergy 4.
References & source
[1]. Brust TF, et al. Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties. Sci Signal. 2017 Feb 21;10(467).
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.