产品描述:
TGR5 is a transmembrane G protein-coupled receptor that is activated by bile acid.{29321} INT-777 is a semisynthetic bile acid that acts as an agonist of TGR5 (EC50 = 0.82 µM).{17880,29490} It is active in vivo, stimulating the secretion of glucagon-like peptide 1 (GLP-1) in mice when given orally (30 mg/kg) after a glucose challenge, particularly when given with a dipeptidyl-peptidase-4 inhibitor.{29490} INT-777 increases energy expenditure and reduces hepatic steatosis and adiposity in mice subjected to diet-induced obesity.{29490} It also stimulates insulin secretion in pancreatic β-cells, reduces inflammation and inhibits atherosclerosis in mice, and promotes chloride secretion through cystic fibrosis transmembrane conductance regulator (CFTR) in Calu-3 airway epithelial cells.{29487,29489,29486}