GPR55 Receptor Antagonist; CID16020046

Biochem/physiol Actions

Primary TargetGPR55

General description

A selective antagonist of G protein-coupled receptor 55 (GPR55) that blocks lipid L-a-lysophosphatidylinositol (LPI, Cat. No. 440153)-induced GPR55 activation (IC₅₀ = 1 µM) and downstream effects in HEK293 cells. Also shown to block the agonistic effect of LPI on GPR55- expressing yeast cells (~10 µM). 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 (~10 µM). Also reported to inhibit the activity of phosphodiesterases PDE3A and PDE4B (pIC₅₀ = 5 and 4.8, respectively).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kargl, J., et al, 2013. J. Pharmacol. Exp. Ther.346, 54.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)