85-2073-19　GPR55 Receptor Antagonist, CID16020046 (4-[4-(3-Hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1H,4H-pyrrolo[3,4-c]pyrazol-5-yl]benzoic Acid) 10mg　217395

特徴

• 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 -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.