An agonist of TGR5 (EC50 = 0.82 µM); stimulates the secretion of GLP-1 in mice when given orally (30 mg/kg) after a glucose challenge

INT-777 – 500 µg

Brand:
Cayman
CAS:
1199796-29-6
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

An agonist of TGR5 (EC50 = 0.82 µM); stimulates the secretion of GLP-1 in mice when given orally (30 mg/kg) after a glucose challenge, particularly when given with a DPP4 inhibitor; increases energy expenditure and reduces hepatic steatosis and adiposity in mice subjected to diet-induced obesity

Formal name: (3α,5β,6α,7α,12α,23S)-6-ethyl-3,7,12-trihydroxy-cholane-23-carboxylic acid

Synonyms:  ​HY-15677|6-EMCA|S-EMCA

Molecular weight: 450.7

CAS: 1199796-29-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Endocrinology & Metabolism|Bile Acids & Microbiome||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity||Research Area|Immunology & Inflammation

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