MilliporeSigma™ Calbiochem™ TGR5 Receptor Agonist, Cpd23g

Description

• A cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC 50 = 720 pM and 6.2nM for human and mouse TGR5, respectively)
• Does not exhibit any significant affinity towards other related targets such as GPR40, GPR119, and GPR120
• Shown to increase glucagon-like peptide-1 (GLP-1) secretion in a dose-dependent manner and significantly reduce blood glucose levels in db/db mice following a single oral dose (50mg/kg)
• Exhibits desirable pharmacokinetic properties in rodent models (t½ = 1.5 h, Cmax = 56 ng/ml; and AUC = 147 ng.h/ml following an oral dose of 5mg/kg).