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Selective 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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 425.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.35 mL||11.75 mL||23.51 mL|
|5 mM||0.47 mL||2.35 mL||4.7 mL|
|10 mM||0.24 mL||1.18 mL||2.35 mL|
|50 mM||0.05 mL||0.24 mL||0.47 mL|
References are publications that support the biological activity of the product.
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
Stančić et al (2015) The GPR55 antagonist CID16020046 protects against intestinal inflammation. Neurogastroenterol.Motil 27 1432 PMID: 26227635
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Keywords: CID 16020046, CID 16020046 supplier, CID16020046, GPR55, antagonists, cannabinoid, ERK1/2, ERK, receptors, 4959, Tocris Bioscience
4 Citations for CID 16020046
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
Shi (2017) The novel cannabinoid receptor GPR55 mediates anxiolytic-like effects in the medial orbital cortex of mice with acute stress. Mol Brain 10 38 PMID: 28800762
Drzazga (2017) Lysophosphatidylcholine elicits intracellular calcium signaling in GPR55-dependent manner Biochem Biophys Res Commun 489 242 PMID: 28552522
Musella (2017) A novel crosstalk within the endocannabinoid system controls GABA transmission in the striatum. Sci Rep 7 7363 PMID: 28779174
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