GPR55 RECEPTOR ANTAGONIST CID16020046 (C005B-228744)

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).

Biochem/physiol Actions

Primary Target
GPR55

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 425.44. Empirical Formula: C₂₅H₁₉N₃O₄. Assay: ≥. 99% (HPLC). Quality Level: 100. form: powder. potency: 1 . μ. M IC₅₀. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. SMILES string: CC1: CC: C(C: C1)C2: NNC3: C2C(N(C3: O)C4: CC: C(C: C4)C(: O)O)C5: CC(: CC: C5)O. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.