S83035 |
TUG-891 |
源叶(MedMol) | 99% |
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- 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
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