A selective antagonist of G protein-coupled receptor 55 (GPR55) that blocks lipid L-a-lysophosphatidylinositol (LPI)-induced GPR55 activation (IC50 = 1uM) and downstream effects in HEK293 cells. Also shown to block the agonistic effect of LPI on GPR55- expressing yeast cells (~10uM). 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 (~10uM). Also reported to inhibit the activity of phosphodiesterases PDE3A and PDE4B (pIC50 = 5 and 4.8, respectively). Molecular Formula: C25H19N3O4 Solubility: DMSO Primary Target: GPR55 Primary Target IC50: 1u Storage and Stability: Store at -20C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Purity:
99% (HPLC)
Form:
Supplied as an off-white powder.
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