TUG891 是一种选择性的长链游离脂肪酸受体 4 (FFA4/GPR120) 的激动剂。

TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids.

TUG-891 displays similar signaling properties to the LCFA α-linolenic acid at human FFA4, 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[1].

Inhibition of recombinant human Mps1 by BAY 1161909 or BAY 1217389 is assessed in TRFRET-based in vitro kinase assays via phosphorylation of a biotinylated peptide (Biotin-Ahx-PWDPDDADITEILG-NH2). Under standard assay conditions kinase and test compound are preincubated for 15 min before enzyme reaction is started by addition of substrate and ATP upon 10 μM[1].

1374516-07-0

C23H21FO3

364.416

TUG 891;TUG891

DMSO:36.4 mg/mL(100 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years