1402602-05-4Relevant articles and documents
Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy
Hansen, Steffen V. F.,Christiansen, Elisabeth,Urban, Christian,Hudson, Brian D.,Stocker, Claire J.,Due-Hansen, Maria E.,Wargent, Ed T.,Shimpukade, Bharat,Almeida, Reinaldo,Ejsing, Christer S.,Cawthorne, Michael A.,Kassack, Matthias U.,Milligan, Graeme,Ulven, Trond
supporting information, p. 2841 - 2846 (2016/04/10)
The free fatty acid receptor 1 (FFA1 or GPR40) is established as an interesting potential target for treatment of type 2 diabetes. However, to obtain optimal ligands, it may be necessary to limit both lipophilicity and polar surface area, translating to a need for small compounds. We here describe the identification of 24, a potent FFA1 agonist with low lipophilicity and very high ligand efficiency that exhibit robust glucose lowering effect.