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

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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 (98):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P2278
    PEN (human)
    		Agonist 99.52%
    PEN (human), one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
    PEN (human)
  • HY-156830
    TGR5 Receptor Agonist 4
    		Agonist 98.95%
    TGR5 Receptor Agonist 4 is an agonist of Bile Acid Receptor (TGR5), with EC50 for hTGR5 and mTGR5 of 2 nM and 3 nM, respectively. TGR5 Receptor Agonist 4 plays important roles in hypoglycemic and weight loss.
    TGR5 Receptor Agonist 4
  • HY-N0593S1
    Deoxycholic acid-d5
    		Activator 99.90%
    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-156830A
    (4′R)-TGR5 Receptor Agonist 4
    		99.90%
    (4′R)-TGR5 Receptor Agonist 4 is the R enantiomer of TGR5 Receptor Agonist 4 (HY-156830). TGR5 Receptor Agonist 4 is an agonist of Bile Acid Receptor (TGR5), with EC50 for hTGR5 and mTGR5 of 2 nM and 3 nM, respectively. TGR5 Receptor Agonist 4 plays important roles in hypoglycemic and weight loss.
    (4′R)-TGR5 Receptor Agonist 4
  • HY-B1899R
    Taurodeoxycholic acid (Standard)
    		Agonist
    Taurodeoxycholic acid (Standard) is the analytical standard of Taurodeoxycholic acid. This product is intended for research and analytical applications. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent. Taurodeoxycholic acid is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholic acid is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholic acid (TDCA) exhibits anti-inflammatory and neuroprotective effects[1][2][3][9][10].
    Taurodeoxycholic acid (Standard)
  • HY-15677A
    INT-777 (R-enantiomer)
    		Agonist
    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-120565
    WB403
    		Activator 99.16%
    WB403 is an orally active TGR5 activator with an EC50 of 5.5 μM against human TGR5. WB403 activates TGR5 to stimulate downstream signaling pathways, promote GLP-1 secretion, improve glucose tolerance in mice with type 2 diabetes, and reduce levels of fasting blood glucose, postprandial blood glucose and HbA1c. WB403 increases pancreatic β-cell mass and restores the distribution of α-cells and β-cells in islets. WB403 is applicable to the research of type 2 diabetes.
    WB403
  • HY-128853S
    Taurodeoxycholate-d6 sodium
    		Agonist 99.4%
    Taurodeoxycholate-d6 sodium salt is a bile salt-related anionic detergent. Taurodeoxycholate-d6 sodium salt is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholate-d6 sodium salt is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate-d6 (TDCA) exhibits anti-inflammatory and neuroprotective effects.
    Taurodeoxycholate-d<sub>6</sub> sodium
  • 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-142159
    FXR/TGR5 agonist 1
    		Agonist 98.03%
    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-147086
    CAY10789
    		Agonist 99.84%
    CAY10789 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-N0593S2
    Deoxycholic acid-d6
    		Activator 99.70%
    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-N1423S1
    Glycocholic acid-d5
    		Activator 99.9%
    Glycocholic acid-d5 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-d<sub>5</sub>
  • 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-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-W089835R
    Sodium taurodeoxycholate hydrate (Standard)
    		Activator
    Sodium taurodeoxycholate hydrate (Standard) is the analytical standard of Sodium taurodeoxycholate hydrate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-178477
    LIFR/GPBAR1 modulator 1
    		Agonist
    LIFR/GPBAR1 modulator 1 is an orally active, potent GPBAR1 agonist (EC50 = 0.2 μM) and LIFR inhibitor (IC50 = 7.9 μM). LIFR/GPBAR1 modulator 1 upregulates leukaemia inhibitory factor (LIF)-mediated mRNA expression of LIFR and GPBAR1 and significantly reduces the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ), and reduces TIMP1 expression and increases MMP9 expression. LIFR/GPBAR1 modulator 1 can be used for the study of human fibrotic disorders.
    LIFR/GPBAR1 modulator 1