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Submit ReviewCID 16020046
Description: Selective GPR55 antagonist
Chemical Name: 4-[4,6-Dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]benzoic acid
Purity: ≥98% (HPLC)
Biological Activity for CID 16020046
CID 16020046 is a 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 for CID 16020046
CID 16020046 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CID 16020046
| M. Wt | 425.44 |
| Formula | C25H19N3O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CID 16020046
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.54 | 100 |
Preparing Stock Solutions for CID 16020046
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 |
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Product Datasheets for CID 16020046
References for CID 16020046
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
If you know of a relevant reference for CID 16020046, please let us know.
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Keywords: CID 16020046, CID 16020046 supplier, CID16020046, GPR55, antagonists, cannabinoid, ERK1/2, ERK, receptors, 4959, Tocris Bioscience
6 Citations for CID 16020046
Citations are publications that use Tocris products. Selected citations for CID 16020046 include:
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
Ken et al (2021) THC Reduces Ki67-Immunoreactive Cells Derived from Human Primary Glioblastoma in a GPR55-Dependent Manner. Cancers (Basel) 13 PMID: 33802282
Hofmann et al (2015) The GPR 55 agonist, L-α-lysophosphatidylinositol, mediates ovarian carcinoma cell-induced angiogenesis. Br J Pharmacol 172 4107 PMID: 25989290
Katarzyna et al (2015) Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures. Neural Plast 2015 130639 PMID: 26090232
Do you know of a great paper that uses CID 16020046 from Tocris? Please let us know.
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Literature in this Area
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Cannabinoid Receptor Ligands Scientific Review
Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.