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Submit ReviewCID 16020046
说明： Selective GPR55 antagonist
化学名： 4-[4,6-Dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]benzoic acid
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for CID 16020046
CID 16020046 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for CID 16020046
| 分子量 | 425.44 |
| 公式 | C25H19N3O4 |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CID 16020046
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 42.54 | 100 |
制备储备液 for CID 16020046
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for CID 16020046
参考文献 for CID 16020046
参考文献是支持产品生物活性的出版物。
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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关键词: CID 16020046, CID 16020046 supplier, CID16020046, GPR55, antagonists, cannabinoid, ERK1/2, ERK, receptors, 4959, Tocris Bioscience
6 篇 CID 16020046 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CID 16020046 的部分引用包括：
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
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
Ken et al (2021) THC Reduces Ki67-Immunoreactive Cells Derived from Human Primary Glioblastoma in a GPR55-Dependent Manner. Cancers (Basel) 13 PMID: 33802282
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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该领域的文献
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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.