中文名称: GTPL5846
英文名称: GTPL5846
CAS No: 83797-69-7
分子式: C12H21N3O2
分子量: 239.32
G10236 GTPL5846 ≥98%(HPLC) (psaitong)
包装规格:
1mg 5mg 10mg 25mg in glass bottle
产品简介:
一种GPR84激动剂,在PI assay中EC50值为105nM。
溶解性:
溶于DMSO(25mg/mL 超声)
储备液保存:
-80°C, 2 years
-20°C, 1 year
靶点:
ERK
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.
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.
保存条件:
-20℃
注意事项:
1、为了您的安全和健康,请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
UN码:
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安全说明:
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