1390641-87-8Relevant academic research and scientific papers
Free fatty acid receptor 1 (FFA1/GPR40) agonists: Mesylpropoxy appendage lowers lipophilicity and improves ADME properties
Christiansen, Elisabeth,Due-Hansen, Maria E.,Urban, Christian,Grundmann, Manuel,Schr?der, Ralf,Hudson, Brian D.,Milligan, Graeme,Cawthorne, Michael A.,Kostenis, Evi,Kassack, Matthias U.,Ulven, Trond
experimental part, p. 6624 - 6628 (2012/09/21)
FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.
