Cat. No. 4959
Chemical Name: 4-[4,6-Dihydro-4-(3-hydroxyphenyl)-
Biological ActivitySelective GPR55 antagonist. Inhibits LPI-induced Ca2+ signaling (IC50 = 0.21 μM in HEK-GPR55 cells), ERK1/2 phosphorylation and GPR55-mediated transcription factor activation. Displays weak inhibition of acetylcholinesterase, μ-opioid receptor, KCNH2 and hERG. Decreases LPI-induced GPR55 internalization. Reduces experimental intestinal inflammation in mice.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Stančić et al (2015) The GPR55 antagonist CID16020046 protects against intestinal inflammation. Neurogastroenterol.Motil 27 1432. PMID: 26227635.
Kargl et al (2013) A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J.Pharmacol.Exp.Ther. 346 54. PMID: 23639801.
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Citations are publications that use Tocris products. Selected citations for CID 16020046 include:
Hofmann et al (2015) The GPR 55 agonist, L-α-lysophosphatidylinositol, mediates ovarian carcinoma cell-induced angiogenesis. Br J Pharmacol 172 4107. PMID: 25989290.
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Keywords: CID 16020046, supplier, CID16020046, GPR55, antagonists, cannabinoid, ERK1/2, ERK, receptors, Tocris Bioscience, GPR55 Antagonist products