1206629-48-2Relevant academic research and scientific papers
Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability
Christiansen, Elisabeth,Due-Hansen, Maria E.,Urban, Christian,Grundmann, Manuel,Schmidt, Johannes,Hansen, Steffen V. F.,Hudson, Brian D.,Zaibi, Mohamed,Markussen, Stine B.,Hagesaether, Ellen,Milligan, Graeme,Cawthorne, Michael A.,Kostenis, Evi,Kassack, Matthias U.,Ulven, Trond
supporting information, p. 982 - 992 (2013/03/28)
The free fatty acid receptor 1 (FFA1, also known as GPR40) mediates enhancement of glucose-stimulated insulin secretion and is emerging as a new target for the treatment of type 2 diabetes. Several FFA1 agonists are known, but the majority of these suffer from high lipophilicity. We have previously reported the FFA1 agonist 3 (TUG-424). We here describe the continued structure-activity exploration and optimization of this compound series, leading to the discovery of the more potent agonist 40, a compound with low lipophilicity, excellent in vitro metabolic stability and permeability, complete oral bioavailability, and appreciable efficacy on glucose tolerance in mice.
COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES
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Page/Page column 89, (2010/04/03)
There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type Il diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
