6-OAU
(Synonyms: GTPL5846) 目录号 : GC11350
6-OAU是G蛋白偶联受体84（GPR84）的特异性激动剂，可以诱导PMNs（polymorphonuclear leukocytes）和巨噬细胞的趋化以及巨噬细胞的促炎反应。
Cas No.:83797-69-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
6-OAU is a specific agonist of G protein-coupled receptor 84 (GPR84) [1] which can induce chemotaxis of polymorphonuclear leukocytes (PMNs) and macrophages as well as a pro-inflammatory response in macrophages [2]. 6-OAU enhances the inflammatory response in macrophages by upregulating the Akt, ERK, and the nuclear factor κB (NFκB) signaling pathways, which causes an increase in expression of key inflammatory cytokines and chemokines [3]. 6-OAU also has anti-bacterial ability and can be a potential candidate to against brucellosis and possibly other intracellular pathogens or inflammatory diseases [2].
6-OAU (0.01nM~0.1mM; 2h) activated human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105nM in the phosphoinositide accumulation assay (PI assay) [1]; 6-OAU (0~10μM; 4h) increased the secretion of IL-8 from LPS-stimulated human peripheral PMNs [1]; 6-OAU (0.001nM~10mM; 30min) activated GPR84 to bind to the Gαi protein, leaded to an inhibition of the production of cAMP with an EC50 of 14nM in CHO cells transfected with the human GPR84 receptor (GPR84-CHO) [3]; 6-OAU (1μM; 30, 60, 90, 120, and 240min) promoted enhanced expression of inflammatory cytokines and chemokines in LPS pre-treated Bone Marrow-Derived Macrophages (BMDMs) [3]; 6-OAU (2μM; 4h) reduced the number of Brucella abortus and Salmonella adhered to the RAW264.7 cells [2].
6-OAU (10mg/kg; i.v.) leaded to the elevation of chemokine CXCL1 in the serum, triggered an inflammatory response in female Lewis rats [1]; 6-OAU (2μM, 100μL/mouse; one week; i.g.) reduced the proliferation of Brucella in the liver and spleen and enhanced the resistance to Brucella infection [2].
References:
[1] Suzuki M, Takaishi S, Nagasaki M, et al. Medium-chain fatty acid-sensing receptor, GPR84, is a proinflammatory receptor [J]. Journal of Biological Chemistry, 2013, 288(15): 10684-10691.
[2] Reyes A W B, Kim H, Huy T X N, 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 [J]. Microbial Pathogenesis, 2021, 158: 105079.
[3] Recio C, Lucy D, Purvis G S D, et al. Activation of the immune-metabolic receptor GPR84 enhances inflammation and phagocytosis in macrophages [J]. Frontiers in Immunology, 2018, 9: 1419.
6-OAU是G蛋白偶联受体84（GPR84）的特异性激动剂[1]，可以诱导PMNs（polymorphonuclear leukocytes）和巨噬细胞的趋化以及巨噬细胞的促炎反应[2]。6-OAU通过上调Akt、ERK和核因子κB（NFκB）的信号通路，导致关键炎症细胞因子和趋化因子的表达增加，从而增强巨噬细胞的炎症反应[3]。6-OAU还具有抗菌能力，具有成为对抗布鲁氏菌病和其他细胞内病原体或炎症性疾病药物的潜力[2]。
6-OAU（0.01nM~0.1mM；2h）在Gqi5嵌合体存在的情况下，通过PI试验（phosphoinositide accumulation assay）测定在HEK293细胞中激活GPR84的EC50为105nM[1]；6-OAU（0~10μM；4h）可以增加LPS处理的人外周PMNs中IL-8的分泌[1]；6-OAU（0.001nM~10mM；30min）激活GPR84后使其与Gαi蛋白结合，从而抑制cAMP的产生，6-OAU在GPR84-CHO中抑制cAMP产生的EC50为14nM[3]；6-OAU（1μM；30、60、90、120和240min）可以促进LPS处理的BMDMs（bone marrow-derived macrophages）炎症因子和趋化因子的表达增强[3]；6-OAU（2μM；4h）可减少Brucella abortus和Salmonella在RAW264.7细胞上的粘附[2]。
6-OAU（10mg/kg；静脉注射）导致雌性Lewis大鼠血清中趋化因子CXCL1升高，引发炎症反应[1]；6-OAU（2μM, 100μL/只；1周；灌胃）可减少Brucella在肝脏和脾脏的增殖，增强对Brucella感染的抵抗力[2]。
| Cell experiment [1]: | |
Cell lines | RAW264.7 |
Preparation Method | Cells were pretreated with 2μM 6-OAU for 4h (0μM as a control), after washing, cells were infected with Salmonella Typhimurium for 30min. |
Reaction Conditions | 2μM; 4h |
Applications | 6-OAU reduced the number of Salmonella adhered to the cells. |
| Animal experiment [2]: | |
Animal models | Female Lewis rats |
Preparation Method | 6-OAU (1mg/ml), was dissolved in sterile PBS containing 1% rat serum and injected into the jugular vein of rats. Control groups received sterile PBS containing 1% rat serum into the jugular vein. Blood was collected 3h after the 6-OAU injection. |
Dosage form | 10mg/kg; i.v. |
Applications | 6-OAU leaded to the elevation of a chemokine and a rise in the concentration of CXCL1 in serum. |
References: | |
| Cas No. | 83797-69-7 | SDF | |
| 别名 | GTPL5846 | ||
| 化学名 | 6-(octylamino)-2,4(1H,3H)-pyrimidinedione | ||
| Canonical SMILES | O=C1NC(NCCCCCCCC)=CC(N1)=O | ||
| 分子式 | C12H21N3O2 | 分子量 | 239.3 |
| 溶解度 | ≤0.25mg/ml in DMSO;0.25mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.1789 mL | 20.8943 mL | 41.7885 mL |
| 5 mM | 835.8 μL | 4.1789 mL | 8.3577 mL |
| 10 mM | 417.9 μL | 2.0894 mL | 4.1789 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet