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

PDF 0.41 MB

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 (44):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13771
    Ursodeoxycholic acid
    		Agonist ≥98.0%
    Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.
    Ursodeoxycholic acid
  • HY-N0593
    Deoxycholic acid
    		Activator 99.82%
    Deoxycholic acid (cholanoic acid), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5.
    Deoxycholic acid
  • HY-111534
    SBI-115
    		Antagonist 99.22%
    SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
    SBI-115
  • HY-15677
    INT-777
    		Agonist ≥98.0%
    INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
    INT-777
  • HY-N0593A
    Deoxycholic acid sodium salt
    		Activator 99.89%
    Deoxycholic acid sodium salt (sodium deoxycholate), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5.
    Deoxycholic acid sodium salt
  • HY-13771A
    Ursodeoxycholic acid sodium
    		Agonist 99.06%
    Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.
    Ursodeoxycholic acid sodium
  • HY-161817
    TGR5 agonist 5
    		Agonist
    TGR5 agonist 5 (compound K91) is a potent agonist of TGR5, with EC50s of 19 μM and 30 μM in CRE-Luciferase assay anf cAMP accumulation assay, respectively.
    TGR5 agonist 5
  • HY-N0169
    Hyodeoxycholic acid
    		Agonist 99.87%
    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
  • HY-B0575
    Triamterene
    		Inhibitor 99.88%
    Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene is an inhibitor of the TGR5 receptor.
    Triamterene
  • HY-14229
    TGR5 Receptor Agonist
    		Agonist 99.71%
    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
  • HY-12434
    INT-767
    		Agonist 99.81%
    INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
    INT-767
  • HY-N0593S
    Deoxycholic acid-d4
    		Activator 98.0%
    Deoxycholic acid-d4 is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
    Deoxycholic acid-d<sub>4</sub>
  • HY-B1899A
    Taurodeoxycholic acid sodium hydrate
    		Activator ≥98.0%
    Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. Taurodeoxycholic acid sodium hydrate activates the S1PR2 pathway in addition to the TGR5 pathway.
    Taurodeoxycholic acid sodium hydrate
  • HY-110173
    TC-G 1005
    		Agonist 99.83%
    TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
    TC-G 1005
  • HY-P2278
    PEN (human)
    		Agonist 99.68%
    PEN (human), one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
    PEN (human)
  • HY-126855
    Cholic acid 7-sulfate
    		Agonist 99.90%
    Cholic acid 7-sulfate (7-Sulfocholic acid), a metabolite of Cholic acid, is a Takeda G-protein receptor 5 (TGR5) agonist. Cholic acid 7-sulfate can increase Tgr5 expression and induce GLP-1 secretion.
    Cholic acid 7-sulfate
  • HY-101274
    BAR501
    		Agonist ≥98.0%
    BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
    BAR501
  • HY-W089835
    Sodium taurodeoxycholate hydrate
    		Activator
    Sodium taurodeoxycholate hydrate, a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. Sodium taurodeoxycholate hydrate activates the S1PR2 pathway in addition to the TGR5 pathway.
    Sodium taurodeoxycholate hydrate
  • HY-N0593S3
    Deoxycholic acid-13C
    		Activator 98.00%
    Deoxycholic acid-13C is the 13C-labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
    Deoxycholic acid-<sup>13</sup>C
  • HY-102016
    SB756050
    		Agonist 98.49%
    SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
    SB756050