TGR5 Receptor Agonist 3 (Compound 19) 是 G 蛋白偶联胆汁酸受体 1（GPBAR1，TGR5）激动剂软药化合物，具有降低胆囊充盈效果（良好的胆囊安全性），对 hTGR5 和 mTGR5 的EC50分别为 16.4 和 209 nM。

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 EC 50 s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively [1].

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 C max value of 0.003 μg/mL [1]. TGR5 Receptor Agonist 3 (compound 19) can reduce gallbladder-filling and safety in vivo [1].

2643391-08-4

C29H27N3O6

513.54

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years