1374516-07-0

TUG 891 is a potent and selective GPR120 agonist as a new potential target for treatment of type 2 diabetes and metabolic diseases.

TUG-891 is an orally activepotent and selective agonist for human long chain free fatty acid (FFA) receptor FFA4/GPR120 (pEC50 of receptor β-arrestin-2 recruitment = 7.36/FFA4 vs. 4.19/FFA1 HEK transfectants; pEC50 of calcium mobilization = 7.02/FFA4 vs. 5.30/FFA1 transfectants)while exhibiting no activity toward human short-chain FFA receptors FFA2/GPR43 and FFA3/GPR41. TUG-891 also exhibits potent partial agonist activity toward murine FFA4 (pEC50 = 7.7775% efficacy by β-arrestin-2 recruitment assay; pEC50 = 6.89 by calcium mobilization)albeit with a reduced selectivity over mFFA1 (pEC50 = 5.92 by β-arrestin-2 recruitment and 6.41 by by calcium mobilization). When administered via water intake (~20 mg/kg/day)TUG-891 is reported to reverse food intake increases and body weight gains among mice subjected to sleep fragmentationand significantly attenuate visceral white adipose tissue inflammation as well as insulin resistance.''TUG-891a GPR120 agonist he

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