GPR84 antagonist 8
目录号 : GC31712GPR84antagonist8是一种选择性GPR84拮抗剂。
Cas No.:1445846-30-9
Sample solution is provided at 25 µL, 10mM.
GPR84 antagonist 8 is a selective GPR84 antagonist.
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].
[1]. Recio C, et al. Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages. Front Immunol. 2018 Jun 20;9:1419.
Cell experiment: | 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]. |
References: [1]. Recio C, et al. Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages. Front Immunol. 2018 Jun 20;9:1419. |
Cas No. | 1445846-30-9 | SDF | |
Canonical SMILES | O=C1N=C(OCC2OCCOC2)C=C3N1CCC4=C3C=CC(OCC5=NC=CC=C5)=C4 | ||
分子式 | C23H23N3O5 | 分子量 | 421.45 |
溶解度 | DMSO : 5 mg/mL (11.86 mM) | 储存条件 | Store at -20°C |
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制备储备液 | |||
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 |
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