1402601-79-9Relevant academic research and scientific papers
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
, 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.
ORTHO-FLUORO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES
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Page/Page column 36-37, (2012/10/18)
There is provided novel fluoro-substituted 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 II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
