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 (67):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-121238R
    Hyocholic Acid (Standard)
    		Activator
    Hyocholic Acid (Standard) is the analytical standard of Hyocholic Acid. This product is intended for research and analytical applications. Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes [1][2][3].
    Hyocholic Acid (Standard)
  • HY-177050
    RG-239
    		Agonist
    RG-239 is an orally active TGR5 agonist with an EC50 of 120 nM, significantly outperforming Betulinic acid (HY-10529) (EC50 = 1.04 μM). RG-239 demonstrates higher selectivity for TGR5 compared to the FXRα. RG-239 increases mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. RG-239 inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 and microglia cells. RG-239 can be used for the study of type 2 diabetes[1][2][3][4][5].
    RG-239
  • 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-P5084
    Neuromedin S (human)
    		Ligand
    Neuromedin S (human) is a neuropeptide that contains 33 amino acids. Neuromedin S (human)has been identified in the brain as an endogenous ligand for the orphan G-protein coupled receptor (GPCR) FM-4/TGR-1 and acts on the neuromedin U (NMU) receptor 2 (NMUR2) in the regulation of body weight homeostasis.
    Neuromedin S (human)
  • 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-168329
    TGR5 agonist 7
    		Agonist
    TGR5 agonist 7 (Compound 22-Na) is a gut-restricted, orally active agonist for G protein-coupled bile acid receptor TGR5 (GPBAR1 or GPR131) with an EC50 < 1 μM. TGR5 agonist 7 exhibits blood glucose lowering effect in mouse model, and can be used in diabete research.
    TGR5 agonist 7
  • 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-N0169A
    Hyodeoxycholic acid sodium
    		Agonist
    Hyodeoxycholic acid sodium 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 sodium
  • 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.
    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-173466
    LT-188A
    		Agonist
    LT-188A is a potent TGR5 agonist with an EC50 of 23 μM. LT-188A decreases the levels of inflammatory mediators in macrophages.
    LT-188A
  • 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
  • HY-128853R
    Taurodeoxycholate sodium salt (Standard)
    		Agonist
    Taurodeoxycholate sodium salt (Standard) is a bile salt (Standard)-related anionic detergent. Taurodeoxycholate sodium salt (Standard) is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholate sodium salt (Standard) is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) exhibits anti-inflammatory and neuroprotective effects.
    Taurodeoxycholate sodium salt (Standard)
  • HY-N0593B
    Deoxycholic acid sodium hydrate
    		Activator
    Deoxycholic acid (cholanoic acid) sodium hydrate, a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5.
    Deoxycholic acid sodium hydrate
  • HY-B1899AR
    Taurodeoxycholic acid sodium hydrate (Standard)
    		Activator
    (E)-Methyl 4-coumarate (Standard) is the analytical standard of (E)-Methyl 4-coumarate. This product is intended for research and analytical applications. (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as Allium cepa or Morinda citrifolia L. leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
    Taurodeoxycholic acid sodium hydrate (Standard)