gpr40 receptor

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

LY2881835 is a potent and selective GPR40 agonist.

Vincamine (Perval) is a major alkaloid of Vinca minor L., Apocynaceae. It has been used therapeutically as a vasodilator and antihypertensive agent, particularly in cerebrovascular disorders.

GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.

GPR40 Activator 2 is a highly effective activator of the GPR40 receptor.

GPR40 FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40 FFAR1) agonist and allosteric modulator.

HWL-088 is a potent free fatty acid receptor 1 (FFA1 GPR40) agonist. HWL-088 significantly improves glucose tolerance in normal and diabetic models.

Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor.

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

TUG-424 significantly enhances glucose-stimulated insulin secretion at 100 nM. TUG-424 is a potent and selective free fatty acid receptor 1 agonist (EC50: 32 nM).

Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist.

BMS-986118 is a full agonist of GPR40, is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial a

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)

Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1 2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84. J.Pharmacol.Exp.Ther. 357 337 PMID:26962172

SCO-267 is a potent allosteric full agonist of the GPR40 receptor, making it a valuable tool in studying chronic diseases like 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 6 (Compound 7a) is a potent and selective agonist of free fatty acid receptor 1 (FFAR1 or GPR40) with an EC50 of 0.058 μM against GPR40 [1].

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.

AMG 837 hemicalcium is a potent, orally active GPR40 FFA1 partial agonist that inhibits the specific binding of [3H]AMG 837 to the human FFA1 receptor (pIC50: 8.13). It promotes insulin secretion and reduces glucose levels in rodents.

AP5 sodium is a selective, potent, orally active GPR40 receptor agonist that exhibits positive allosteric modulation of endogenous ligands (AgoPAM). sodium exhibits potential for the study of type II diabetes.

Xelaglifam is a potent agonist of G protein-coupled receptor 40 (GPR40) and exhibits hypoglycemic effects.

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.