TUG-891

Catalog No.S6775 Batch:S677501

Technical Data

Formula	C₂₃H₂₁FO₃
Molecular Weight	364.41	CAS No.	1374516-07-0
Solubility (25°C)*	In vitro	Ethanol	36 mg/mL (98.78 mM)
		DMSO	23 mg/mL (63.11 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

TUG-891 is a potent and selective agonist of the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism.

Targets

FFA4/GPR120 ^[1]

In vitro

TUG-891 displays similar signaling properties to the LCFA α-linolenic acid at human FFA4 across various assay end points, including stimulation of Ca_²⁺ 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]

In vivo

TUG-891 acutely increases fat oxidation and reduces body weight and fat mass in C57Bl/6J mice by activating GPR120.^[2]

Protocol (from reference)

Cell Assay:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

References

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SHIPPING AND STORAGE
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