Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes
详细信息 查看全文
- 作者：Elisabeth Christiansen ; Steffen V. F. Hansen ; Christian Urban ; Brian D. Hudson ; Edward T. Wargent ; Manuel Grundmann ; Laura Jenkins ; Mohamed Zaibi ; Claire J. Stocker ; Susanne Ullrich ; Evi Kostenis ; Matthias U. Kassack ; Graeme Milligan ; Michael A. Cawthorne ; Trond Ulven
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：May 9, 2013
- 年：2013
- 卷：4
- 期：5
- 页码：441-445
- 全文大小：301K
- 年卷期：v.4,no.5(May 9, 2013)
- ISSN：1948-5875
文摘
Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic 尾-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.