TUG-891

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Chemical Structure| 1374516-07-0 同义名 : -
CAS号 : 1374516-07-0
货号 : A844329
分子式 : C23H21FO3
纯度 : 99%+
分子量 : 364.41
MDL号 : MFCD22421654
存储条件:

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Fatty acids can be agonists for cell surface G protein–coupled receptors (GPCRs) to regulate metabolic and inflammatory processes. FFA4, a menber of free fatty acid (FFA) receptor family, belongs to GPCRs. TUG-891 is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor FFA4 with pEC50 of 7.22 for hFFA4 which is 288-fold more potent than hFFA1. In Ca2+ mobilization assays employing Flp-In T-REx 293 cells that had been engineered to express human FFA4 (hFFA4), TUG-891 potently produced concentration-dependent increases in intracellular Ca2+. Further, TUG-891 again potently produced concentration-dependent responses in the Ca2+ assays. Again in hFFA4-inducible Flp-In T-REx 293 cells, TUG-891 increased ERK phosphorylation in a clear, concentration-dependent manner. Internalization of hFFA4 was monitored in live cells at 5-minute intervals after treatment with TUG-891 (10 μM). Furthermore, TUG-891 was able to promote desensitization of the receptor-signaling response and phosphorylation of hFFA4. In 3T3-L1 mouse adipocytes model, treatment with TUG-891 (10 μM) produced a statistically significant increase of [3H]deoxyglucose uptake[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL

参考文献

[1]Hudson BD, Shimpukade B, 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]Shimpukade B, Hudson BD, et al. Discovery of a potent and selective GPR120 agonist. J Med Chem. 2012 May 10;55(9):4511-5.

[3]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