Chemical Name: 4-[4,6-Dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]benzoic acid
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.
A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function.
Kargl et al.
The GPR55 antagonist CID16020046 protects against intestinal inflammation.
Stančić et al.
Citations for CID 16020046
The citations listed below are publications that use Tocris products. Selected citations for CID 16020046 include:
4 Citations: Showing 1 - 4
A novel crosstalk within the endocannabinoid system controls GABA transmission in the striatum.
Sci Rep 2017;7(1):7363
Lysophosphatidylcholine elicits intracellular calcium signaling in GPR55-dependent manner
Biochem Biophys Res Commun 2017;489(2):242
The novel cannabinoid receptor GPR55 mediates anxiolytic-like effects in the medial orbital cortex of mice with acute stress.
Mol Brain 2017;10(1):38
The GPR 55 agonist, L-α-lysophosphatidylinositol, mediates ovarian carcinoma cell-induced angiogenesis.
Authors: Hofmann Et al.
Br J Pharmacol 2015;172:4107
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