产品描述: TUG-891是一种有效的、选择性 long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120) 激动剂 |
靶点:
FFA4/GPR120;GPR |
体外研究:
TUG-891 displays similar signaling properties to the LCFA α-linolenic acid at human FFA4 across various assay end points, including stimulation of Ca²⁺ mobilization, β-arrestin-1 and β-arrestin-2 recruitment, and extracellular signal-regulated kinase phosphorylation. Activation of human FFA4 by TUG-891 also results in rapid phosphorylation and internalization of the receptor |
体内研究:
TUG-891 acutely increases fat oxidation and reduces body weight and fat mass in C57Bl/6J mice by activating GPR120 |
细胞实验:
Cell lines: Human FFA4-eYFP Flp-In T-REx cells, HT-29 cells Concentrations: 10 μM Incubation Time: 1.5 min, 5 min, 45 min Method: Intracellular Ca2+ is monitored for 1.5 min after TUG-891 treatment, and the measured response is taken as the peak signal over this time course. Extracellular signal-regulated kinase 1/2 (ERK) phosphorylation is examined in Flp-In T-REx cell lines, or in HT-29 cells after 5 minutes of TUG-891 treatment. For visualization of FFA4 Internalization, human FFA4-eYFP Flp-In T-REx cells are cultured on poly-d-lysine coated glass coverslips and cultured for 24 hours before treatment with doxycycline (100 ng/ml) to induce receptor expression. Live cells are imaged after TUG-891 addition using a confocal microscopy system. |
参考文献:
1. Hudson BD, et al. The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism. Mol Pharmacol. 2013 Nov;84(5):710-25. 2. Schilperoort M, et al. The GPR120 agonist TUG-891 promotes metabolic health by stimulating mitochondrial respiration in brown fat. EMBO Mol Med. 2018 Mar;10(3):e8047. |
溶解性:
Soluble in DMSO、Ethanol |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.744 ml |
13.721 ml |
27.442 ml |
5 mM |
0.549 ml |
2.744 ml |
5.488 ml |
10 mM |
0.274 ml |
1.372 ml |
2.744 ml |
50 mM |
0.055 ml |
0.274 ml |
0.549 ml |
|
注意: |
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