TGR5 Receptor Agonist 3

TGR5 Receptor Agonist 3 (Compound 19) is a soft-drug G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively[1].

Signaling Pathways >> GPCR/G Protein >> GPCR19

Research Areas >> Metabolic Disease

TGR5 Receptor Agonist 3 (compound 19) (10-50μM, 2 hours) activates TGR5 in fetal rat intestinal cells (FRIC) and NCI-H716 cells to promote GLP-1 secretion in a dose-dependent manner[1].

TGR5 Receptor Agonist 3 (compound 19) has good targeting and can effectively activate TGR5, thus promoting the secretion of GLP-1 in plasma and regulating the homeostasis of glucose metabolism in male ICR mice[1]. TGR5 Receptor Agonist 3 (compound 19) can be rapidly absorbed and metabolized in male ICR mice, and has a good safety profile[1]. TGR5 Receptor Agonist 3 (compound 19) (oral gavage; 50 mg/kg; one hour) can be gavaged into overnight-fasted male ICR mice for one hour with a Cmaxvalue of 0.003 μg/mL [1]. TGR5 Receptor Agonist 3 (compound 19) can reduce gallbladder-filling and safety in vivo[1].

[1]. Fanghui Han, et al. Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects. Eur J Med Chem. 2020 Oct 1;203:112619.