Biological Activity
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.
Compound Libraries
CID 16020046 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 425.44 |
| Formula | C25H19N3O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 834903-43-4 |
| PubChem ID | 16020046 |
| InChI Key | VGUQVYZXABOXCX-UHFFFAOYSA-N |
| Smiles | O=C1N(C5=CC=C(C(O)=O)C=C5)C(C4=CC=CC(O)=C4)C2=C1NN=C2C3=CC=C(C)C=C3 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.54 | 100 |
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 solvent 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: CID 16020046, supplier, CID16020046, GPR55, antagonists, cannabinoid, ERK1/2, ERK, receptors, GPR55, GPR55, Tocris Bioscience
