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• 产品描述： 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

• 靶点： ERK;GPR

• 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. Cell Viability Assay Cell Line: B. abortus Concentration: 0, 0.02, 0.2, 2 μM Incubation Time: 0, 2, 24, 48, 72 hours Result: Decreased B. abortus survivability begin at 48 h with a dose of 2 μM. Western Blot Analysis Cell Line: RAW264.7 cells infected with B. abortus Concentration: 2 μM Incubation Time: 4 hours Result: Reduced ERK phosphorylation and MALT1 expression in RAW264.7 macrophag

• 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.

• 参考文献：
  1. Suzuki M, et al. Medium-chain fatty acid-sensing receptor, GPR84, is a proinflammatory receptor. J Biol Chem. 2013 Apr 12;288(15):10684-91. 2. Reyes AWB, et al. Immune-metabolic receptor GPR84 surrogate and endogenous agonists, 6-OAU and lauric acid, alter Brucella abortus 544 infection in both in vitro and in vivo systems. Microb Pathog. 2021 Sep. 158:105079.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	4.179 ml	20.893 ml	41.786 ml
  5 mM	0.836 ml	4.179 ml	8.357 ml
  10 mM	0.418 ml	2.089 ml	4.179 ml
  50 mM	0.084 ml	0.418 ml	0.836 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *