gpr40 agonist 2

GPR40 Agonist 2 is a compound that functions as a GPR40 agonist and is utilized in diabetes research.

LY2881835 is a potent and selective GPR40 agonist.

GPR40 agonist 1 is an effective new GPR40 agonist (EC50s: 17 nM and 2 nM for rGPR40 and hGPR40).

LY2922470 reduces glucose levels along with significant enhancements in insulin and GLP-1, which is the potential for the treatment of type 2 diabetes mellitus (T2DM). LY2922470 is an effective, selective, and orally available agonist of the G protein-cou

ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. 1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020)

ZQ-16 is a potent and highly selective agonist for the G protein-coupled receptor GPR84, demonstrating a half-maximal effective concentration (EC50) of 0.213 μM, and it activates multiple downstream signaling pathways including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of extracellular signal-regulated protein kinase 1/2 (ERK1/2), receptor desensitization and internalization, and receptor-β-arrestin interaction, making it a useful tool compound for studying GPR84 function and a candidate for further optimization.

SCO-267 is a full agonist of GPR40/FFAR1 with an EC50 of 12 nM, effectively stimulating insulin secretion and GLP-1 release in diabetic rats, improving glucose tolerance, and can be used for the treatment of type 2 diabetes.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist (EC50: 7.39). It shows higher affinity for FFAR1 or GPR40 relative to related receptors FFA2, FFA3, and the nuclear receptor PPARγ, as well as various other receptors, ion channels, and transporter proteins. TUG-499 is useful for studying Type 2 diabetes.

GPR40 agonist 5 is an orally active GPR40 (G protein-coupled receptor 40) agonist (EC50: 47 nM). gPR40 agonist 5 reduces blood glucose levels and improves glucose tolerance. gPR40 agonist 5 shows adequate control of hyperglycemic state in type 2 diabetic mice.

MK-8666 Tris is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 Tris has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.

MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.

BI-2081, a GPR40 (FFAR1) partial agonist with an EC50 of 4 nM, promotes glucose-dependent insulin secretion and lowers plasma glucose levels. This compound is utilized in metabolic disease research, specifically targeting type 2 diabetes.

CPL207280, an orally active GPR40 FFA1 agonist with antidiabetic effects, enhances glucose-stimulated insulin secretion and improves glucose tolerance in MIN6 pancreatic β-cells, healthy Wistar Han rats, and diabetic rat models, making it a valuable compound for type 2 diabetes research [1] [2].

TUG-770 is a GPR40 FFA1 agonist with potential anti-inflammatory activity.TUG-770 can be used to study type 2 diabetes, dementia, and Alzheimer's disease.