A FFAR4 agonist
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TUG-891

Item No. 17035

Technical Information
Formal Name
4-[(4-fluoro-4'-methyl[1,1'-biphenyl]-2-yl)methoxy]-benzenepropanoic acid
CAS Number
1374516-07-0
Molecular Formula
C23H21FO3
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 1 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.1 mg/mlEthanol: 1 mg/ml
SMILES
CC1=CC=C(C2=CC=C(F)C=C2COC3=CC=C(CCC(O)=O)C=C3)C=C1
InChi Code
InChI=1S/C23H21FO3/c1-16-2-7-18(8-3-16)22-12-9-20(24)14-19(22)15-27-21-10-4-17(5-11-21)6-13-23(25)26/h2-5,7-12,14H,6,13,15H2,1H3,(H,25,26)
InChi Key
LPGBXHWIQNZEJB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TUG-891 is an agonist of free fatty acid receptor 4 (FFAR4/GPR120; EC50s = 0.0436 and 0.0169 µM for the human and mouse receptors, respectively).1 It is selective for FFAR4 over FFAR1/GPR40 (EC50 = 64.5 µM for the human receptor) and is inactive against FFAR2/GPR43 and FFAR3/GPR41. TUG-891 (1 µM) inhibits lysophosphatidic acid- or EGF-induced proliferation and migration of DU145 and PC3 prostate cancer cells.2 It stimulates glucagon-like peptide 1 (GLP-1) release in STC-1 enteroendrocrine cells and glucose uptake in 3T3-L1 adipocytes, as well as inhibits LPS-induced TNF-α release in RAW 264.7 macrophages when used at a concentration of 10 µM.3 TUG-891 (20 mg/kg) reduces sleep fragmentation-induced increases in food consumption and epididymal fat mass in mice.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shimpukade, B., Hudson, B.D., Hovgaard, C.K., et alDiscovery of a potent and selective GPR120 agonist. J. Med. Chem. 55(9), 4511-4515 (2012).

    2. Liu, Z., Hopkins, M.M., Zhang, Z., et alOmega-3 fatty acids and other FFA4 agonists inhibit growth factor signaling in human prostate cancer cells. J. Pharmacol. Exp. Ther. 352(2), 380-394 (2015).

    3. Hudson, B.D., Shimpukade, B., Mackenzie, A.E., et alThe 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. 84(5), 710-725 (2013).

    4. Gozal, D., Qiao, Z., Almendros, I., et alTreatment with TUG891, a free fatty acid receptor 4 agonist, restores adipose tissue metabolic dysfunction following chronic sleep fragmentation in mice. Int. J. Obes. (Lond.) 40(7), 1143-1149 (2016).