TGR5 Receptor Agonist, Cpd23g

A cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC₅₀ = 720 pM and 6.2 nM 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 (50 mg/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 5 mg/kg).

A cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC₅₀ = 720 pM and 6.2 nM 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 (50 mg/kg). Exhibits desirable pharmacokinetic properties in rodent models (t1/2 = 1.5 h, Cmax = 56 ng/ml; and AUC = 147 ng.h/ml following an oral dose of 5 mg/kg).

Primary Target
TGR5

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Duan, H., et al. 2012, J. Med. Chem.55, 10475.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany