TGR5 Receptor Agonist 3 

TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent 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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

513.54

C₂₉H₂₇N₃O₆

2643391-08-4

CCOCOC(C1=COC2=C1C=C(C=C2)OC3=C(C=NC=C3)C(N4CCN(C5=C4C=CC=C5)C6CC6)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]