1. Signaling Pathways
  2. GPCR/G Protein
  3. GPCR19

GPCR19

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.

GPCR19 Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-15677
    INT-777
    Agonist ≥98.0%
    INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
  • HY-N0593
    Deoxycholic acid
    Activator ≥98.0%
    Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-111534
    SBI-115
    Antagonist 99.57%
    SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
  • HY-14229
    TGR5 Receptor Agonist
    Agonist 99.85%
    TGR5 Receptor Agonist (CCDC), a potent TGR5(GPCR19) agonist, shows improved potency in the U2-OS cell assay (pEC50=6.8) and in melanophore cells (pEC50=7.5).
  • HY-B0575
    Triamterene
    Inhibitor 99.98%
    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.
  • HY-N0593A
    Deoxycholic acid sodium salt
    Activator ≥98.0%
    Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-N0169
    Hyodeoxycholic acid
    Agonist ≥99.0%
    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.
  • HY-101274
    BAR501
    Agonist ≥98.0%
    BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
  • HY-12434
    INT-767
    Agonist ≥98.0%
    INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
  • HY-102016
    SB756050
    Agonist 99.32%
    SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
  • HY-101273
    BAR502
    Agonist ≥98.0%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  • 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.
  • HY-110173
    TC-G 1005
    Agonist 99.91%
    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.
  • HY-P2277
    PEN (rat)
    Agonist
    PEN (rat), one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
  • HY-P2278
    PEN (human)
    Agonist
    PEN (human), one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
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