Christiansen, Elisabeth3; Hansen, Steffen V F3; Urban, Christian2; Hudson, Brian D2; Wargent, Edward T2; Grundmann, Manuel2; Jenkins, Laura2; Zaibi, Mohamed2; Stocker, Claire J2; Ullrich, Susanne2; Kostenis, Evi2; Kassack, Matthias U2; Milligan, Graeme2; Cawthorne, Michael A2; Ulven, Trond3
1 Department of Physics, Chemistry and Pharmacy, Faculty of Science, SDU2 unknown3 Department of Physics, Chemistry and Pharmacy, Faculty of Science, SDU
A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes
Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.
A C S Medicinal Chemistry Letters, 2013, Vol 4, Issue 5, p. 441-445