| 產(chǎn)品描述： | TUG-891是一種有效的、選擇性 long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120) 激動(dòng)劑 |
| 靶點(diǎn)： |
FFA4/GPR120;GPR |
| 體外研究： |
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 |
| 體內(nèi)研究： |
TUG-891 acutely increases fat oxidation and reduces body weight and fat mass in C57Bl/6J mice by activating GPR120 |
| 細(xì)胞實(shí)驗(yàn)： |
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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京