TGR5 agonist 9 is a highly selective and orally active TGR5 allosteric agonist with EC₅₀ values for hTGR5 and mTGR5 of 0.48 and 0.49 μM, respectively. TGR5 agonist 9 can recruit β-arrestin 1 ( EC₅₀ = 78.8 μM) and β-arrestin 2 ( EC₅₀ = 12.3 μM), and has a higher efficacy in cAMP accumulation ( EC₅₀ = 0.48 μM). TGR5 agonist 9 exhibits a significant hypoglycemic effect in the ICR mouse model. TGR5 agonist 9 can be used for research on diabetes.
Products | Products > Disease Areas > Metabolic or Endocrine Disease | Products > Disease Areas > Glucose Metabolism | Products > Signaling Pathways > GPCR/G Protein | Products > Research Areas > Metabolic Disease | Products > Signaling Pathways > G protein-coupled Bile Acid Receptor 1
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