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 |
|---|---|---|---|---|
|
V12282 | BAR-501 | 1632118-69-4 | BAR-501 is a selective GPBAR1 agonist devoid of any FXR agonistic activity. |
|
V29159 | Hyodeoxycholic acid | 83-49-8 | Hyodeoxycholic acid (HDCA), a secondary metabolite of bile acid and one of the metabolic byproducts produced by intestinal bacteria, is TGR5 (GPCR19) agonist (EC50 = 0.82 μM). |
|
V4823 | SBI-115 | 882366-16-7 | SBI-115 (SBI115) is a novel and potent TGR5 (GPCR19) antagonist with the potential to be used for polycystic liver disease. |
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