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CAS No. : 83797-69-7
MCE 国际站:6-OAU
产品活性:6-OAU (GTPL5846) 是一种 GPR84 (G 蛋白偶联受体 84) 激动剂,EC50 为 105 nM。6-OAU 对中性粒细胞和巨噬细胞都有趋化作用,并扩增促炎细胞因子 IL-8,表现出促炎功能。6-OAU 还具有抗细菌感染能力。
研究领域:GPCR/G Protein | Stem Cell/Wnt | MAPK/ERK Pathway | Anti-infection
作用靶点:GPR84 | ERK | Bacterial | Antibiotic
In Vitro: GPR84 gene exhibits high expression in human polymorphonuclear leukocytes (PMNs) and macrophages, 6-OAU acts on proinflammatory function by activitating GPR84.
6-OAU (0.01 nM-0.1 mM; 1 h) activates human GPR84 in the presence of Gqi5 chimera with an EC50 value of 105 nM in HEK293 cells.
6-OAU (0, 6.25, 200 μM; 30 min) stimulates [35S]GTP binding, accumulates phosphoinositides, and induces GPR84-EGFP internalization in a GPR84-dependent manner.
6-OAU (1 nM-1 mM; 1 h) provokes chemotaxis of PMNs in a concentration-dependent manner with an EC50 value of 318 nM.
6-OAU (0-10 μM; 4 h) increases the secretion of IL-8 from LPS-stimulated PMNs.
6-OAU (0-0.4 μM; 16 h) also amplifies TNF-α production from U937 macrophages.
6-OAU (2 μM; 4 h) decreases ERK phosphorylation and MCP-1 protein expression, (2 μM; 48 h) decreases MCP-1 secretion in macrophages .
6-OAU (2 μM; 24 h) reduces ROS production during B. abortus infection in RAW264.7 cells.
6-OAU (2 μM; 0, 30, and 60 min) inhibits adhesion and Brucella uptake in RAW264.7 cells and (2 μM; 30 min) shows anti-infection against Brucella and Salmonella infection.
In Vivo: 6-OAU activates GPR84 and results in making an inflammatory condition through chemokine production and chemotaxis in vivo.
6-OAU (10 mg/kg; i.v.) raises the blood CXCL1 level in rats.
6-OAU (1 mg/mL; s.c.) attracts both PMNs and macrophages into the air pouch.
6-OAU (2 μM, 100 mL/mouse; s.c.) augments resistance to Brucella infection, and reduces bacterial proliferation in spleens and livers.
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