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 (45):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P2277
    PEN (rat)
    		Agonist 99.24%
    PEN (rat), one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
    PEN (rat)
  • HY-15677A
    INT-777 (R-enantiomer)
    		Agonist 98.73%
    INT-777 (R-enantiomer) is the R-enantiomer of INT-777, with EC50 of 4.79 μM for TGR5, and less potent than INT-777.
    INT-777 (R-enantiomer)
  • HY-147086
    CAY10789
    		Agonist 99.84%
    CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.
    CAY10789
  • HY-B0575R
    Triamterene (Standard)
    		Inhibitor 99.92%
    Triamterene (Standard) is the analytical standard of Triamterene. This product is intended for research and analytical applications. Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene as an inhibitor of the TGR5 receptor.
    Triamterene (Standard)
  • HY-101273
    BAR502
    		Agonist 99.53%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
    BAR502
  • HY-145234
    GPBAR1-IN-3
    		Agonist
    GPBAR1-IN-3 (Compound 14) is a selective GPBAR1 agonist (EC50=0.17 μM) and a CysLT1R antagonist.
    GPBAR1-IN-3
  • HY-P2277A
    PEN (rat) (TFA)
    		Agonist
    PEN (rat) TFA, one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
    PEN (rat) (TFA)
  • HY-107612
    GPBAR-A
    		Agonist
    GPBAR-A is a specific agonist of the bile acid receptor GPBAR1. GPBAR-A can be used for the research of diabetes mellitus.
    GPBAR-A
  • HY-N0593S1
    Deoxycholic acid-d5
    		Activator
    Deoxycholic acid-d5 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>5</sub>
  • HY-139677A
    5-HT7R antagonist 1 free base
    		Antagonist
    5-HT7R antagonist 1 (free base) is a G protein-biased antagonist against 5-HT7R (Ki = 6.5 nM).
    5-HT7R antagonist 1 free base
  • HY-149807
    TGR5 agonist 1
    		Agonist
    TGR5 agonist 1 (compound 18) is a potent TGR5 agonist with an EC50 value of 0.31 µM.
    TGR5 agonist 1
  • HY-142159
    FXR/TGR5 agonist 1
    		Agonist
    FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the research of fatty liver disease.
    FXR/TGR5 agonist 1
  • HY-133862
    SCH-202676
    		Modulator
    SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 µM.
    SCH-202676
  • HY-N0593S2
    Deoxycholic acid-d6
    		Activator
    Deoxycholic acid-d6 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>6</sub>
  • HY-13771S1
    Ursodeoxycholic acid-13C
    		Agonist
    Ursodeoxycholic acid-13C is the 13C labeled Ursodeoxycholic acid. 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. Orally active[1][2].
    Ursodeoxycholic acid-<sup>13</sup>C
  • HY-146453
    TGR5 Receptor Agonist 3
    		Agonist
    TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.
    TGR5 Receptor Agonist 3
  • HY-155307
    TGR5 agonist 4
    		Agonist
    TGR5 agonist 4 (compound 19), a cholic acid derivative, is a selective TGR5 agonist with an EC50 of 4 μM.
    TGR5 agonist 4
  • HY-116453
    RO5527239
    		Agonist
    RO5527239 is an orally active TGR5 agonist, that induces a stimulatory response from intestinal L cells and specificially secrets the endogenous hormone GLP-2.
    RO5527239
  • HY-139677
    5-HT7R antagonist 1
    		Antagonist
    5-HT7R antagonist 1 is a G protein-biased antagonist against 5-HT7R (Ki = 6.5 nM).
    5-HT7R antagonist 1
  • HY-149808
    TGR5 agonist 2
    		Agonist
    TGR5 agonist 2 (compound 19) is a potent TGR5 agonist with an EC50 value of 0.27 µM.
    TGR5 agonist 2