6-OAU (GTPL5846) 是一种GPR84(G 蛋白偶联受体 84) 激动剂，EC50为 105 nM。6-OAU 对中性粒细胞和巨噬细胞都有趋化作用，并扩增促炎细胞因子 IL-8，表现出促炎功能。6-OAU 还具有抗细菌感染能力。
| 生物活性 | 6-OAU (GTPL5846) (6-n-octylaminouracil) is anGPR84(G protein-coupled receptor 84) agonist, with anEC50value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokineIL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function[1][2]. |
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体外研究
(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 Gqi5chimera with an EC50value 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 EC50value 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 againstBrucellaandSalmonellainfection[2].
Cell Viability Assay[2] | 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[2] | 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 macrophages. |
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体内研究
(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].
| Animal Model: | Female Lewis rats(4-week-old)[1] | | 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)[1] | | 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)[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(104.47 mM;Need ultrasonic) 配制储备液 | 1 mM | 4.1787 mL | 20.8934 mL | 41.7868 mL | | 5 mM | 0.8357 mL | 4.1787 mL | 8.3574 mL | | 10 mM | 0.4179 mL | 2.0893 mL | 4.1787 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
