TGR5 agonist 9 is a selective allosteric agonist targeting the TGR5 receptor, exhibiting EC₅₀ values of 0.48 μM for human and murine TGR5. This compound effectively recruits β-arrestin 1 and β-arrestin 2, with EC₅₀ values of 78.8 μM and 12.3 μM, respectively, and demonstrates notable efficacy in cAMP accumulation. In the ICR mouse model, TGR5 agonist 9 shows significant hypoglycemic effects, making it a valuable tool for research related to diabetes.
TGR5 agonist 9 is a selective allosteric agonist targeting the TGR5 receptor, exhibiting EC₅₀ values of 0.48 μM for human and murine TGR5. This compound effectively recruits β-arrestin 1 and β-arrestin 2, with EC₅₀ values of 78.8 μM and 12.3 μM, respectively, and demonstrates notable efficacy in cAMP accumulation. In the ICR mouse model, TGR5 agonist 9 shows significant hypoglycemic effects, making it a valuable tool for research related to diabetes.
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