6-OAU (GTPL5846) (6-n-octylaminouracil) functions as a GPR84 (G protein-coupled receptor 84) agonist with an EC50 of 105 nM. It attracts PMNs and macrophages, boosts IL-8 proinflammatory cytokine levels, indicating its proinflammatory effects. Additionally, 6-OAU has antibacterial capabilities[1][2].
体内研究
6-OAU triggers GPR84, leading to the creation of an inflammatory state via chemokine production and chemotaxis in vivo[1].
6-OAU (10 mg/kg; i.v.) elevates the blood CXCL1 concentration in rats[1].
6-OAU (1 mg/mL; sC.) draws both PMNs and macrophages into the air pouch[1].
6-OAU (2 μM, 100 mL/mouse; subcutaneously) enhances resistance to Brucella infection and diminishes bacterial growth in spleens and livers[2].
体外研究
The GPR84 gene is highly expressed in human polymorphonuclear leukocytes (PMNs) and macrophages, with 6-OAU promoting proinflammatory activity through activation of GPR84[1].
6-OAU (0.01 nM-0.1 mM; 1 h) triggers human GPR84 activation when combined with Gqi5 chimera, achieving an EC50 of 105 nM in HEK293 cells[1].
6-OAU (0, 6.25, 200 μM; 30 min) promotes [35S]GTP binding, leads to phosphoinositide accumulation, and causes GPR84-EGFP to internalize in a manner dependent on GPR84[1].
6-OAU (1 nM-1 mM; 1 h) induces PMNs chemotaxis in a concentration-dependent fashion, achieving an EC50 of 318 nM[1].
6-OAU (2 μM; 4 h) reduces ERK phosphorylation and MCP-1 protein expression, while (2 μM; 48 h) lowers MCP-1 secretion in macrophages[2].
6-OAU (2 μM; 24 h) diminishes ROS output during B. abortus infection in RAW264.7 cells[2].
6-OAU (2 μM; 0, 30, and 60 min) impedes adhesion and Brucella absorption in RAW264.7 cells, and (2 μM; 30 min) exhibits anti-infective properties against Brucella and Salmonella infections[2].
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