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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V121587 | (4′R)-TGR5 Receptor Agonist 4 | 1872436-55-9 | (4′R)-TGR5 Receptor Agonist 4 is the R enantiomer of TGR5 receptor agonist 4. |
|
V121668 | (7α,24S)-7,24-Dihydroxycholest-4-en-3-one | 2260669-16-5 | (7α,24S)-7,24-Dihydroxycholest-4-en-3-one is an oxosterol. |
|
V124539 | 2-Bromo-LSD D-Tartrate | 2855123-30-5 | 2-Bromo-LSD D-Tartrate is a partial agonist and competitive partial antagonist of the 5-HT2A receptor that can cross the blood-brain barrier. |
|
V125529 | 3-MPPI | 133399-65-2 | 3-MPPI is a G protein-coupled receptor (GPCR) ligand with high selectivity for α1-adrenergic receptors. Its Ki value for α1-adrenergic receptors is 0.21 nM, and its Ki value for 5-HT1A receptors is 50 nM. |
|
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). |
|
V127387 | 6ECA | 647011-80-1 | 6ECA is a selective TGR5 receptor activator with an EC50 value of 3.44 μM. |
|
V129213 | AP-503 | 767299-99-0 | AP-503 is a selective GPR133/ADGRD1 agonist with an EC50 of 1.21 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. | |
|
V131650 | Cholic acid 7-sulfate-d4 | 1332881-66-9 | Cholic acid 7-sulfate-d4 is a deuterated derivative of 7-sulfocholic acid. |
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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. |
|
V76959 | GRK2i TFA | GRK2i TFA is a GRK2 inhibitory peptide that specifically inhibits Gβγ activation of GRK2. | |
|
V79649 | GRL018-21 | GRL018-21 is a potent and selective G protein-coupled receptor kinase 5 (GRK5) inhibitor (antagonist) with IC50 of 10 nM. | |
|
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). | |
|
V139100 | LT-188A | 2922530-99-0 | LT-188A is a potent TGR5 agonist with an EC50 of 23 μM. |
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V141564 | Norhyodeoxycholic acid | 77518-23-1 | Norhyodeoxycholic acid is a synthetic bile acid and a derivative of porcine deoxycholic acid (HDCA). |
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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. |
|
V142414 | PEN (human) TFA | PEN (human) TFA is one of the most abundant neuropeptides in the hypothalamus, derived from the proprotein ProSAAS, and is an endogenous ligand of GPR83. | |
|
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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