G protein-coupled Bile Acid Receptor 1
G-protein coupled receptor 19; GPCR19; TGR5; GPBAR1
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.
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G protein-coupled Bile Acid Receptor 1 Ligands
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G protein-coupled Bile Acid Receptor 1 Related Products (99)
Related Products (99)
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5-HT7R antagonist 1
0 ImagesCat. No.: HY-139677CAS No.: 2759919-13-45-HT7R antagonist 1 is a G protein-biased antagonist against 5-HT7R (Ki = 6.5 nM).
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TGR5 agonist 2
0 ImagesCat. No.: HY-149808CAS No.: 3027426-06-5TGR5 agonist 2 (compound 19) is a potent TGR5 agonist with an EC50 value of 0.27 µM.
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Allolithocholic Acid-d4
0 ImagesCat. No.: HY-143712S1Synonyms: 3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4Allolithocholic Acid-d4 (3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease.
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Deoxycholic acid sodium hydrate
0 ImagesCat. No.: HY-N0593BCAS No.: 145224-92-6Synonyms: Cholanoic Acid sodium hydrate; Desoxycholic acid sodium hydrateDeoxycholic acid (cholanoic acid) sodium hydrate, a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5.
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Glycocholic acid sodium (Standard)
0 ImagesCat. No.: HY-N1423ARCAS No.: 863-57-0Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium 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 sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
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3-MPPI
0 ImagesCat. No.: HY-101008CAS No.: 133399-65-23-MPPI is a GPCR ligand with high selectivity for α1-adrenergic receptor, with a Ki value of 0.21 nM for α1-adrenergic receptor and 50 nM for 5-HT1A receptor. 3-MPPI modulates the α1-adrenergic receptor signaling cascade. 3-MPPI is applicable to research related to hypertension, stress-induced anxiety-like behavioral responses, and levodopa-induced dyskinesia.
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Taurodeoxycholic acid sodium hydrate (Standard)
0 ImagesCat. No.: HY-B1899ARCAS No.: 110026-03-4Synonyms: Taurodeoxycholate sodium hydrate (Standard)(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.
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TGR5 agonist 3
0 ImagesCat. No.: HY-155306CAS No.: 2148317-51-3TGR5 agonist 3 (compound 8), a Cholic acid derivative, is a selective TGR5 agonist with an EC50 of 5 μM.
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Taurodeoxycholat-d4 sodium
0 ImagesCat. No.: HY-128853S1Taurodeoxycholat-d4 sodium is the deuterium labeled Taurodeoxycholate sodium (HY-128853). Taurodeoxycholate sodium salt is a bile salt-related anionic detergent. Taurodeoxycholate sodium salt is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholate sodium salt is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) exhibits anti-inflammatory and neuroprotective effects.
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6ECA
0 ImagesCat. No.: HY-41333CAS No.: 647011-80-16ECA is a selective TGR5 receptor activator with an EC50 of 3.44 μM. 6ECA shows no significant activity at FXR. 6ECA can be used for the study of diabesity.
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TGR5 agonist 1
0 ImagesCat. No.: HY-149807CAS No.: 3027426-02-1TGR5 agonist 1 (compound 18) is a potent TGR5 agonist with an EC50 value of 0.31 µM.
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SBI-115 (Standard)
0 ImagesCat. No.: HY-111534RCAS No.: 882366-16-7
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Cholic acid 7-sulfate-d4
0 ImagesCat. No.: HY-126855SCAS No.: 1332881-66-9Synonyms: 7-Sulfocholic acid-d4Cholic acid 7-sulfate-d4 (7-Sulfocholic acid-d4) is the deuterium labeled Cholic acid 7-sulfate (HY-126855). Cholic acid 7-sulfate is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation.
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TGR5 agonist 10
0 ImagesCat. No.: HY-181102CAS No.: 3081614-92-5TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes.
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TGR5 agonist 6
0 ImagesCat. No.: HY-168140CAS No.: 2925211-47-6TGR5 agonist 6 (compund 22b) is a non-systemic gut-targeted TGR5 agonist with significant and sustained blood sugar-lowering effects and an acceptable safety profile.
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TGR5 agonist 9
0 ImagesCat. No.: HY-180845CAS No.: 2931879-67-1TGR5 agonist 9 is a highly selective and orally active TGR5 allosteric agonist with EC₅₀ values for hTGR5 and mTGR5 of 0.48 and 0.49 μM, respectively. TGR5 agonist 9 can recruit β-arrestin 1 (EC₅₀ = 78.8 μM) and β-arrestin 2 (EC₅₀ = 12.3 μM), and has a higher efficacy in cAMP accumulation (EC₅₀ = 0.48 μM). TGR5 agonist 9 exhibits a significant hypoglycemic effect in the ICR mouse model. TGR5 agonist 9 can be used for research on diabetes.
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TGR5 Receptor Agonist (Standard)
0 ImagesSynonyms: CCDC (Standard)TGR5 Receptor Agonist (Standard) is the analytical standard of TGR5 Receptor Agonist. This product is intended for research and analytical applications. 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.
