TGR5 agonist 10 is a selective, allosteric agonist of the Takeda G protein-coupled receptor 5 (TGR5), exhibiting EC50 values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. This compound uniquely activates both human and mouse TGR5, leading to increased cAMP accumulation, while exhibiting higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 modulates the functional activity of lithocholic acid and has demonstrated glucose-lowering effects in oral glucose tolerance tests in Mus musculus. It is an important tool for research into diabetes and metabolic disorders.
TGR5 agonist 10 is a selective, allosteric agonist of the Takeda G protein-coupled receptor 5 (TGR5), exhibiting EC50 values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. This compound uniquely activates both human and mouse TGR5, leading to increased cAMP accumulation, while exhibiting higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 modulates the functional activity of lithocholic acid and has demonstrated glucose-lowering effects in oral glucose tolerance tests in Mus musculus. It is an important tool for research into diabetes and metabolic disorders.
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