Home GPCR & G Protein Cannabinoid Receptor antagonist CID16020046

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CID16020046 Cannabinoid Receptor antagonist

Cat.No.S8694

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 Cannabinoid Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 425.44

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 425.44 Formula

C25H19N3O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 834903-43-4 -- Storage of Stock Solutions

Synonyms C390-0219 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

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
GPR55 [2]
(in yeast)
0.15 μM
In vitro

In yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney (HEK293) cells stably expressing human GPR55, this 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). It 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].
In vivo

CID16020046 improves inflammation in models of intestinal inflammation and reduces proinflammatory cytokines. This compound does not change the locomotor and anxiety behavior of healthy mice[1].
References

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