6-OAU (Synonyms: GTPL5846) |
| رقم الكتالوجGC11350 |
6-OAU (GTPL5846) (6-n-octylaminouracil) هو ناهض GPR84 (مستقبلات مقترنة بالبروتين 84) ، بقيمة EC50 تبلغ 105 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| المرادفات | GTPL5846 | ||
| Chemical Name | 6-(octylamino)-2,4(1H,3H)-pyrimidinedione | ||
| Canonical SMILES | O=C1NC(NCCCCCCCC)=CC(N1)=O | ||
| Formula | C12H21N3O2 | M.Wt | 239.3 |
| الذوبان | ≤0.25mg/ml in DMSO;0.25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *