CAS 3081614-92-5

TGR5 agonist 10

CAS : 3081614-92-5

TGR5 agonist 10 is a selective, allosteric, and orally bioavailable agonist for the Takeda G protein-coupled receptor 5 (TGR5), with EC₅₀ values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. It demonstrates specificity for TGR5 over FXR and can activate both human and mouse TGR5 to induce cAMP accumulation. The compound enhances cholic acid's functional activity and efficacy on hTGR5 and shows higher selectivity in cAMP formation compared to β-arrestin 2 recruitment. TGR5 agonist 10 exhibits hypoglycemic effects in an oral glucose tolerance test in Mus musculus and can be utilized in diabetes research.

Formule : C₂₅H₄₀O₆

Masse moléculaire : 436.58

Ref: TM-T218011