2. Signaling Pathways
  3. GPCR/G Protein
  4. G protein-coupled Bile Acid Receptor 1

G protein-coupled Bile Acid Receptor 1

G-protein coupled receptor 19; GPCR19; TGR5; GPBAR1

G protein-coupled Bile Acid Receptor 1

Related Products

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G protein-coupled bile acid receptor 1 (GPCR19, TGR5, GPBAR1) is a plasma membrane-bound, G protein-coupled receptor that has bile acids as its ligand. GPCR19 is a regulator of energy homeostasis, bile acid homeostasis as well as glucose metabolism. GPCR19 transduces extracellular signals through heterotrimeric G proteins.

GPCR19 can be activated by bile acids and then it induces cAMP production. As a membrane receptor, GPCR19 can be internalized into the cytoplasm in response to its ligands. GPCR19 plays important roles in cell signaling pathways such as nuclear factor κB (NF-κB), AKT, and extracellular signal-regulated kinases (ERK). Its agonists may be potential drugs for the treatment of metabolic, inflammation, and digestive disorders. In addition, GPCR19 stimulates glucagon-like peptide 1 (GLP-1) secretion. It also has become an attractive therapeutic target for the prevention and/or the treatment of obesity and its highly associated Type II diabetes and metabolic syndrome.

G protein-coupled Bile Acid Receptor 1 Related Products (67):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0169S
    Hyodeoxycholic acid-d5
    		Agonist
    Hyodeoxycholic acid-d5 is the deuterium labeled Hyodeoxycholic acid. Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
    Hyodeoxycholic acid-d<sub>5</sub>
  • HY-155306
    TGR5 agonist 3
    		Agonist
    TGR5 agonist 3 (compound 8), a Cholic acid derivative, is a selective TGR5 agonist with an EC50 of 5 μM.
    TGR5 agonist 3
  • HY-101274A
    (3α,5β,6β,7α)-BAR501
    		≥98.0%
    (3α, 5β, 6β, 7α)-BAR501 (BAR504-6b) is a compound having cholane scaffolds of formula. (3α, 5β, 6β, 7α)-BAR501 can be used for the research of FXR and TGR5/GPBAR1 mediated diseases.
    (3α,5β,6β,7α)-BAR501
  • HY-120565
    WB403
    		Activator
    WB403 is a TGR5 activator. WB403 promotes GLP-1 release, improved hyperglycemia, and preserves the mass and function of pancreatic β-cells.
    WB403
  • HY-126855S
    Cholic acid 7-sulfate-d4
    		Agonist
    Cholic acid 7-sulfate-d4 (7-Sulfocholic acid-d4) is the deuterium labeled Cholic acid 7-sulfate (HY-126855). Cholic acid 7-sulfate is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation.
    Cholic acid 7-sulfate-d<sub>4</sub>
  • HY-168140
    TGR5 agonist 6
    		Agonist
    TGR5 agonist 6 (compund 22b) is a non-systemic gut-targeted TGR5 agonist with significant and sustained blood sugar-lowering effects and an acceptable safety profile.
    TGR5 agonist 6
  • HY-14229R
    TGR5 Receptor Agonist (Standard)
    		Agonist
    TGR5 Receptor Agonist (Standard) is the analytical standard of TGR5 Receptor Agonist. This product is intended for research and analytical applications. TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity.
    TGR5 Receptor Agonist (Standard)