48 products were found matching "K08400"!

The gene GPBRA1 encodes G protein-coupled bile acid receptor. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production.

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,...

Dehydrolithocholic acid is a major metabolite of lithocholic acid (LCA, Cay-20253). It is formed from LCA by the cytochrome P450 (CYP) isoform CYP3A4. Dehydrolithocholic acid is an agonist of G protein-coupled bile acid activated receptor 1 (GP-BAR1/TGR5, EC50 = 0.27 µM), vitamin D receptor (VDR, EC50 = 3 µM), and...

5beta-Cholestane-3alpha,7alpha,12alpha,25-tetrol is a bile acid alcohol. It induces activation of G protein-coupled bile acid receptor 1 (GPBAR1), also known as TGR5, in HEK293 cells expressing the human receptor when used at concentrations ranging from 0. to 10 µM. Blood, fecal, and bile levels of...

TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays). It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM). TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose...

Betulinic acid is a natural plant triterpenoid that is structurally related to mammalian bile acids. It is an agonist of the G protein-coupled bile acid receptor TGR5 (EC50 = 1 µM), which might be linked with its ability to alter gene expression and fatty liver development in cells and mice given ethanol. Betulinic...

Bile acids are a diverse class of amphipathic molecules originally formed in liver and modified by microorganisms in the intestine. In addition to their conventional role in dietary lipid absorption, bile acids have been recognized as signaling molecules that regulate the synthesis and metabolism of bile acids,...

BAR501 is a selective agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1, EC50 = 1 µM) that lacks activity at the farnesoid X receptor (FXR). In vivo, BAR501 reduces hepatic perfusion pressure and counteracts norepinephrine-induced vasoconstriction in naïve rats. It protects against development...

TGR5 agonist.

SBI-115 is an antagonist of G protein-coupled bile acid receptor 1 (GPBAR1), also known as TGR5. It inhibits taurolithocholic acid-induced increases in cAMP levels in, and proliferation of, cholangiocytes isolated from patients with autosomal dominant polycystic kidney disease when used at concentrations of 100 and...

Anti-BG37 Antibody is sera. A BLAST analysis was used to suggest cross-reactivity with BG37 from human and mouse based on 100% homology with the immunizing sequence. Predicted reactivity with cow. Cross-reactivity with BG37 from other sources has not been determined. Protein function: Receptor for bile acid. Bile...

BAR502 is a dual agonist of the G protein-coupled bile acid-activated receptor and farnesoid x receptor (GP-BAR1 and FXR, EC50s = 0.2 and 1 µM, respectively). It increases the expression of the FXR-regulated bile salt export pump (BSEP), organic solute transporter alpha (OSTalpha), and small heterodimer partner...