INT-777

TGR5 is a transmembrane G protein-coupled receptor that is activated by bile acid. INT-777 is a semisynthetic bile acid that acts as an agonist of TGR5 (EC50 = 0.82 µM). 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. INT-777 increases energy expenditure and reduces hepatic steatosis and adiposity in mice subjected to diet-induced obesity. It also stimulates insulin secretion in pancreatic beta-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.Formal Name: (3alpha,5beta,6alpha,7alpha,12alpha,23S)-6-ethyl-3,7,12-trihydroxy-cholane-23-carboxylic acid. CAS Number: 1199796-29-6. Synonyms: 6-EMCA, S-EMCA, HY-15677. Molecular Formula: C27H46O5. Formula Weight: 450.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL, DMSO: 20 mg/mL, Ethanol: 25 mg/mL. SMILES: O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])C[C@H](O)[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@H](C)C[C@H](C)C(O)=O)([H])C1. InChi Code: InChI=1S/C27H46O5/c1-6-17-20-12-16(28)9-10-26(20,4)21-13-22(29)27(5)18(14(2)11-15(3)25(31)32)7-8-19(27)23(21)24(17)30/h14-24,28-30H,6-13H2,1-5H3,(H,31,32)/t14-,15+,16-,17-,18-,19+,20+,21+,22+,23+,24-,26+,27-/m1/s1. InChi Key: NPBCMXATLRCCLF-IRRLEISYSA-N.