Bile acids serve as the ligand for the plasma membrane-bound G protein-coupled bile acid receptor 1 (GPCR19, TGR5, GPBAR1). Energy homeostasis, bile acid homeostasis, and glucose metabolism are all regulated by GPCR19. GPCR19 uses heterotrimeric G proteins to transmit extracellular signals.
Bile acids have the ability to activate GPCR19, which then triggers the production of cAMP. GPCR19 is a membrane receptor that, in response to ligands, can internalize into the cytoplasm. GPCR19 is crucial for cell signaling pathways like nuclear factor-B (NF-B), extracellular signal-regulated kinases (ERK), and akt (AKT). Potential medications for the treatment of digestive, inflammatory, and metabolic disorders include its agonists. Additionally, GPCR19 promotes the release of the hormone glucagon-like peptide 1 (GLP-1). It has also developed into a desirable therapeutic target for the prevention and/or treatment of obesity, Type II diabetes, and the metabolic syndrome, which are all closely related to obesity.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V75364 | 5-HT7R antagonist 1 | 2759919-13-4 | 5-HT7R antagonist 1 is a G protein-biased antagonist of 5-HT7R (Ki = 6.5 nM). |
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V75362 | 5-HT7R antagonist 1 free base | 2337008-64-5 | 5-HT7R antagonist 1 (free base) is a G protein-biased antagonist of 5-HT7R (Ki = 6.5 nM). |
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V77161 | CCG258208 hydrochloride (GRK2-IN-1 hydrochloride) | CCG258208 (GRK2-IN-1) HCl is a potent and specific inhibitor of GRK2 (G protein-coupled receptor kinase 2) (IC50=30 nM), showing 230-fold activity against GRK5 (IC50=7.09 μM) The selectivity is over 2500-fold for GRK1 (IC50=87.3 μM), PKA and ROCK1. | |
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V74029 | FXR/TGR5 agonist 1 | 2677689-72-2 | FXR/TGR5 agonist 1 has agonistic effects on FXR and TGR5 and may be utilized to study fatty liver disease. |
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V75361 | GPBAR1-IN-3 | 2760546-05-0 | GPBAR1-IN-3 (Compound 14) is a selective GPBAR1 agonist (EC50=0.17 μM) and CysLT1R antagonist. |
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V76959 | GRK2i TFA | GRK2i TFA is a GRK2 inhibitory peptide that specifically inhibits Gβγ activation of GRK2. | |
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V79649 | GRL018-21 | GRL018-21 is a potent and selective G protein-coupled receptor kinase 5 (GRK5) inhibitor (antagonist) with IC50 of 10 nM. | |
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V116577 | LIFR/GPBAR1 modulator 1 | LIFR/GPBAR1 modulator 1 is an orally effective potent GPBAR1 agonist (EC50 = 0.2 μM) and LIFR inhibitor (IC50 = 7.9 μM). | |
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V75360 | PEN (human) | 597578-70-6 | PEN (human) is one of the most abundant hypothalamic neuropeptides derived from ProSAAS proprotein and is the endogenous ligand of GPR83. |
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V75363 | PEN (rat) | 569364-13-2 | PEN (rat) is one of the most abundant hypothalamic neuropeptides derived from ProSAAS proprotein and is the endogenous ligand of GPR83. |
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V81076 | PEN (rat) (TFA) | PEN (rat) TFA is one of the most abundant hypothalamic neuropeptides derived from ProSAAS proprotein and is the endogenous ligand of GPR83. | |
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V15922 | TC-G 1005 | 1415407-60-1 | TC-G 1005 (TC-G-1005; TCG1005) is a novel, oral and potent TGR5 (GPBAR1) agonist with glucose-lowering effects. |
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V81565 | TGR5 agonist 1 | TGR5 agonist 1 (compound 18) is a potent TGR5 agonist with EC50 of 0.31 µM. | |
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V81566 | TGR5 agonist 2 | TGR5 agonist 2 (compound 19) is a potent TGR5 agonist with EC50 of 0.27 µM. | |
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V75358 | TGR5 agonist 3 | 2148317-51-3 | TGR5 agonist 3 (compound 8) is a cholic acid analogue and a selective TGR5 agonist/activator with EC50 of 5 μM. |
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V78995 | TGR5 agonist 4 | TGR5 agonist 4 (compound 19) is a cholic acid analogue and a selective TGR5 agonist/activator with EC50 of 4 μM. | |
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V86606 | TGR5 agonist 5 | TGR5 agonist 5 (compound K91) is a potent agonist of TGR5 with EC50 of 19 μM and 30 μM in CRE-Luciferase assay and cAMP accumulation assay, respectively. | |
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V94900 | TGR5 agonist 6 | 2925211-47-6 | TGR5 agonist 6 (compound 22b) is a non-systemic gut-targeted TGR5 agonist with significant and sustained hypoglycemic effects and an acceptable safety profile. |
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V110739 | TGR5 agonist 8 | The EC50 value of TGR5 agonist 8 (compound 7i) is 571 nM. | |
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V110043 | TGR5 agonist 9 | 2931879-67-1 | TGR5 agonist 9 is a highly selective, orally effective TGR5 allosteric agonist with EC₅₀ values of 0.48 μM and 0.49 μM for hTGR5 and mTGR5, respectively. |
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