Home GPCR & G Protein Cannabinoid Receptor antagonist CID16020046 For research use only.

CID16020046

Synonyms: C390-0219

CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.

CID16020046 Chemical Structure

CID16020046 Chemical Structure

CAS: 834903-43-4

Purity & Quality Control

Batch: S869401 DMSO] 85 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.96%
99.96

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Signaling Pathway

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Cannabinoid Receptor Signaling Pathway

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Biological Activity

Description CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
Targets
GPR55 [2]
(in yeast)
0.15 μM
In vitro
In vitro

In yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney (HEK293) cells stably expressing human GPR55, the compound behaved as an antagonist on LPI-mediated Ca2+ release and extracellular signal-regulated kinases activation, but not in HEK293 cells expressing cannabinoid receptor 1 or 2 (CB1 or CB2). CID16020046 concentration dependently inhibited lysophosphatidylinositol (LPI)-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor κ of activated B cells (NF-κB) and serum response element, translocation of NFAT and NF-κB, and GPR55 internalization[2].
Cell Research Cell lines J774A.1 cells
Concentrations 1, 5 and 10 μM
Incubation Time 30 min
Method

2 × 106 cells were transferred into 500 μL PBS and preincubated for 30 mins with 1, 5, and 10 μM CID16020046 or vehicle (DMSO). Cells were then stimulated with 1 nM of monocyte chemotactic protein 1 (MCP-1) for another 30 mins at 37°C. Alexa Fluor 647 anti-mouse CD11b was added 15 min before the end of the incubation time. After adding the fixative solution, cells were measured on a FACSCalibur flow cytometer. Experiments were performed in triplicates and data were expressed as percentage change to the vehicle treatment.
In Vivo
In vivo

CID16020046 improves inflammation in models of intestinal inflammation and reduces proinflammatory cytokines. CID16020046 does not change the locomotor and anxiety behavior of healthy mice[1].
Animal Research Animal Models C57BL/6 mice
Dosages 20 mg/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 425.44 Formula

C25H19N3O4
CAS No. 834903-43-4 SDF --
Smiles CC1=CC=C(C=C1)C2=NNC3=C2C(N(C3=O)C4=CC=C(C=C4)C(=O)O)C5=CC(=CC=C5)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (199.79 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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