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NCG21 is a GPR120 agonist. NCG21 showed potent extracellular signal-regulated kinase (ERK) activation in a cloned GPR120 system. NCG21 potently activated ERK, intracellular calcium responses and GLP-1 secretion in murine enteroendocrine STC-1 cells that express GPR120 endogenously. Moreover, administration of NCG21 into the mouse colon caused an increase in plasma GLP-1 levels. | [Uses]
GPR120 Agonist 5 (compound 12) is an agonist targeting GPR120 (EC50=1.2 μM). GPR120 Agonist 5 promotes the release of glucagon-like 1 (GLP-1) by binding to the GPR120 receptor, which in turn binds to its receptors on pancreatic beta cells, increasing insulin secretion and thereby lowering blood sugar levels. GPR120 Agonist 5 also helps reduce chronic low-grade inflammation, which plays an important role in the pathogenesis of obesity, insulin resistance, and type 2 diabetes. GPR120 Agonist 5 can be used to investigate the mechanism of action of GPR120 in metabolic and inflammatory diseases[1][2]. | [References]
[1] Suzuki T, et al. Identification of G protein-coupled receptor 120-selective agonists derived from PPARγ agonists[J]. Journal of medicinal chemistry, 2008, 51(23): 7640-7644. DOI:10.1021/jm800970b
[2] Shimpukade B, et al. Discovery of a potent and selective GPR120 agonist[J]. Journal of medicinal chemistry, 2012, 55(9): 4511-4515. DOI:10.1021/jm300215x |
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