1082058-85-2Relevant academic research and scientific papers
COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES
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Page/Page column 37, (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.
Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths
Comin, Maria J.,Czifra, Gabriella,Kedei, Noemi,Telek, Andrea,Lewin, Nancy E.,Kolusheva, Sofiya,Velasquez, Julia F.,Kobylarz, Ryan,Jelinek, Raz,Blumberg, Peter M.,Marquez, Victor E.
experimental part, p. 3274 - 3283 (2010/03/05)
Diacylglycerol lactones built with a rigid 4-[(methylphenyl)ethynyl]phenyl rod that is separated from the exocyclic acylcarbonyl of the DAG-lactone core by a spacer unit of variable length were synthesized and studied. Binding affinities for a panel of cl
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA1/GPR40), a potential target for the treatment of type II diabetes
Christiansen, Elisabeth,Urban, Christian,Merten, Nicole,Liebscher, Kathrin,Karlsen, Kasper K.,Hamacher, Alexandra,Spinrath, Andreas,Bond, Andrew D.,Drewke, Christel,Ullrich, Susanne,Kassack, Matthias U.,Kostenis, Evi,Ulven, Trond
supporting information; experimental part, p. 7061 - 7064 (2009/11/30)
A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA1) has been discovered and explored. The preferred compound 20 (TUG-424, EC50 = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity.
