6-OAU

6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC₅₀ value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function^[1][2]. IC50 & Target:EC50: 105 nM (GPR84)^[1] In Vitro:GPR84 gene exhibits high expression in human polymorphonuclear leukocytes (PMNs) and macrophages, 6-OAU acts on proinflammatory function by activitating GPR84^[1].
6-OAU (0.01 nM-0.1 mM; 1 h) activates human GPR84 in the presence of G_qi5 chimera with an EC₅₀ value of 105 nM in HEK293 cells^[1].
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^[1].
6-OAU (1 nM-1 mM; 1 h) provokes chemotaxis of PMNs in a concentration-dependent manner with an EC₅₀ value of 318 nM^[1].
6-OAU (0-10 μM; 4 h) increases the secretion of IL-8 from LPS-stimulated PMNs^[1].
6-OAU (0-0.4 μM; 16 h) also amplifies TNF-α production from U937 macrophages^[1].
6-OAU (2 μM; 4 h) decreases ERK phosphorylation and MCP-1 protein expression, (2 μM; 48 h) decreases MCP-1 secretion in macrophages ^[2].
6-OAU (2 μM; 24 h) reduces ROS production during B. abortus infection in RAW264.7 cells^[2].
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^[2]. In Vivo:6-OAU activates GPR84 and results in making an inflammatory condition through chemokine production and chemotaxis in vivo^[1].
6-OAU (10 mg/kg; i.v.) raises the blood CXCL1 level in rats^[1].
6-OAU (1 mg/mL; s.c.) attracts both PMNs and macrophages into the air pouch^[1].
6-OAU (2 μM, 100 mL/mouse; s.c.) augments resistance to Brucella infection, and reduces bacterial proliferation in spleens and livers^[2].