MilliporeSigma™ Calbiochem™ GPR55 Receptor Antagonist, CID16020046

Description

• A selective antagonist of G protein-coupled receptor 55 (GPR55) that blocks lipid L-a-lysophosphatidylinositol (LPI, Cat
• No
• 440153)-induced GPR55 activation (IC 50 = 1μM) and downstream effects in HEK293 cells
• Also shown to block the agonistic effect of LPI on GPR55- expressing yeast cells (∽10μM)
• Inhibits LPI-induced Ca2+ mobilization and ERK1/2 phosphorylation in HEK-GPR55 and HEK-CB1 cells
• However, it does not affect basal Ca2+ mobilization and ERK1/2 activity
• Blocks the GPR55-mediated NFAT and NF-kB activation and their nuclear translocation in HEK-GPR55 cells
• Diminishes LPI-induced wound healing in GPR55-expressing primary human lung microvascular endothelial cells and reverses LPI-inhibited platelet aggregation (∽10μM)
• Also reported to inhibit the activity of phosphodiesterases PDE3A and PDE4B (pIC 50 = 5 and 4.8, respectively).