Formulation: A crystalline solid
Formal Name: (3α,5β,6α,7α,12α,23S)-6-ethyl-3,7,12-trihydroxy-cholane-23-carboxylic acid
Purity: ≥95%
Formula Markup: C27H46O5
Formula Weight: 450,7
Shelf life (days): 1460
CAS Number: 1199796-29-6
Notes: 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}
English
Deutsch
