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Discovery of a potent and selective GPR120 agonist.

Journal of medicinal chemistry (2012-04-24)
Bharat Shimpukade, Brian D Hudson, Christine Kiel Hovgaard, Graeme Milligan, Trond Ulven
ABSTRACT

GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.

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Sigma-Aldrich
TUG-891, ≥98% (HPLC)