1. GPCR/G Protein
  2. GPR84

GPR84 antagonist 8 

Cat. No.: HY-112562 Purity: 99.96%
Handling Instructions

GPR84 antagonist 8 is a selective GPR84 antagonist.

For research use only. We do not sell to patients.

GPR84 antagonist 8 Chemical Structure

GPR84 antagonist 8 Chemical Structure

CAS No. : 1445846-30-9

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Description

GPR84 antagonist 8 is a selective GPR84 antagonist.

IC50 & Target

GPR84[1]

In Vitro

GPR84 is a member of the metabolic G protein-coupled receptor family, and its expression has been described predominantly in immune cells. To test the hypothesis that blocking the activation of GPR84 can be a potential anti-inflammatory strategy in different inflammatory diseases, GPR84 antagonist 8 is used. The potency and specificity of GPR84 antagonist 8 is assessed tusing GPR84-CHO cells in the cAMP assay. GPR84 antagonist 8 effectively inhibits the action of 6-OAU in decreasing cAMP production in GPR84-CHO cells. To test GPR84 antagonist 8’s inhibition of the pro-inflammatory effects of GPR84 activation in macrophages, LPS pre-treated BMDMs are incubated with 10 µM GPR84 antagonist 8 for 30 min before adding 1 µM 6-OAU. Protein analysis by Western Blot shows that the GPR84 antagonist 8 partially blocks the phosphorylation of AKT and ERK induced by 6-OAU[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3728 mL 11.8638 mL 23.7276 mL
5 mM 0.4746 mL 2.3728 mL 4.7455 mL
10 mM 0.2373 mL 1.1864 mL 2.3728 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Bone marrow-derived macrophages treated with either vehicle (0.3% DMSO) or 1 µM 6-OAU for 1 h are incubated with unopsonised pHrodo E. coli bioparticles at 0.1 mg/mL in a 96-well flat clear bottom plate. For the inhibition studies with GPR84 antagonist 8, cells are pretreated with 10 µM GPR84 antagonist 8 for 30 min before addition of either vehicle or 6-OAU. The plate is then placed into the IncuCyte Zoom platform which is housed inside a humidified incubator at 37°C, 5% CO2. Two to four images per well from three technical replicates are taken every 15 min for 4 h[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

421.45

Formula

C₂₃H₂₃N₃O₅

CAS No.

1445846-30-9

SMILES

O=C1N=C(OCC2OCCOC2)C=C3N1CCC4=C3C=CC(OCC5=NC=CC=C5)=C4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GPR84 antagonist 8
Cat. No.:
HY-112562
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GPR84 antagonist 8

Cat. No.: HY-112562