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6-OAU

GPR84的合成激动剂,6-OAU(GTPL5846; 6-n-octylaminouracil)是GPR84激动剂，在PI assay中EC50值为105nM。

目录号: PC11492 纯度: ≥98%

CAS No. :83797-69-7

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中文名称

6-OAU

中文别名

6-(辛基氨基)-2,4(1H,3H)-嘧啶二酮

英文名称

6-OAU

英文别名

6-(octylaMino)pyriMidine-2,4(1H,3H)-dione;GTPL5846;6-OAU;6-n-octylaminouracil;6-(octylamino)-1H-pyrimidine-2,4-dione;2,4(1H,3H)-Pyrimidinedione, 6-(octylamino)-;6-(Octylamino)-2,4(1H,3H)-pyrimidinedione;6-n-octyl aminouracil;AOB5243;BCP14892;BDBM50189502;Q27074016;6-(octylamino)-1,2,3,4-tetrahydropyrimidine-2,4-dione

Cas No.

83797-69-7

分子式

C₁₂H₂₁N₃O₂

分子量

239.31

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

IC50 & Target[1][2]

ERK

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.
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.
6-OAU (0, 6.25, 200 μM; 30 min) stimulates [S]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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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 macrophages.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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 体外研究 and in vivo systems. Microb Pathog. 2021 Sep. 158:105079. [Information]

溶解度数据

体外研究:

DMSO : 25 mg/mL (104.47 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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