产品
编 号:F474197
分子式:C12H21N3O2
分子量:239.31
产品类型
结构图
CAS No: 83797-69-7
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产品详情
生物活性:
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.
体内研究:
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.Animal Model:Female Lewis rats(4-week-old)
Dosage:10 mg/kg
Administration:Intravenous injection; collecting blood 3 h after injection
Result:Increased the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection.
Animal Model:Rat air pouch model (4-week-old female rats)
Dosage:1 mg/mL (PBS)
Administration:Subcutaneous injection; washing the cavity 4 h after injection
Result:Attracted both PMNs and macrophages into the air pouch, peaking at 4 h after the injection.
Animal Model:ICR female mice (7-week-old)
Dosage:2 μM (100 μL/mouse)
Administration:Oral average; 7 days and another 14 days after treated mouse with B. abortus (2 × 105 CFU /100 μL; i.p.)
Result:Reduced bacterial proliferation in the liver and spleen, and decreased IFN-γ but augmented IL-6 serum level.Lowed splenic weight of mice and splenic proliferation.
体外研究:
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.