GPR40 Agonist 2 is a GPR40 agonist. It can be used in the research of diabetes.

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

GPR40 agonist 6 (Compound 7a) is a potent and selective agonist of free fatty acid receptor 1 ( FFAR1 or GPR40 ) with an EC 50 of 0.058 μM against GPR40 [1].

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

GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.

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

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.

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.

LY2881835 is a specific G protein-coupled receptor 40 (GPR40) agonist with potential hypoglycemic activity that enhances glucose-stimulated insulin secretion in normal lean mice.LY2881835 has been used in the study of type 2 diabetes.

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.

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

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist (EC50: 7.39).TUG-499 has an affinity for FFAR1 or GPR40 over the related receptors FFA2, FFA3 and the nuclear receptor PPARγ, as well as other different receptors, ion channels and transporter proteins.TUG-499 can be used to study type 2 Type 2 diabetes.

TAK-875 Hemihydrate (Fasiglifam) is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.

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.

AMG 837 is a partial GPR40 agonist with an EC50 value of 13 nM, showcasing 85% of the maximal activity displayed by DHA in standard assay conditions, indicating its high potency and selectivity in vitro. This compound excels as a GPR40 agonist with a notable pharmacokinetic profile, effectively stimulating insulin secretion in a glucose-dependent manner in rodents and demonstrating potent insulin secretion stimulation in MIN6 cells, with efficacy comparable to that observed in aequorin Ca2+-flux assays. Moreover, AMG 837 exhibits a two-fold increase in potency compared to its racemic counterpart on GPR40, with demonstrated activity across rat and mouse GPR40 versions (EC50 = 23 and 13 nM, respectively). It lacks significant activity against PPARα, δ, and γ in cell-based assays, and an analysis against an external panel of 64 receptors revealed negligible activity, except for a weak inhibition (IC50 = 3 μM) on the a2-adrenergic receptor.

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t

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)

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.

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.

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).

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.

AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavailability. AM-3189 does not penetrate the rat CNS as indicated by a rat brain to plasma ratio of 0.04 at 3 h after an oral dose of 5 mg/kg.

AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM).

AM-4668 is a type 2 diabetes GPR40 agonist. For GPR40, in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), the EC50s are 3.6 nM and 36 nM, respectively.

AS1975063 is a GPR40 agonist.

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

GW-1100 is a selective GPR40 and FFAR1 antagonist for the study of diabetes and metabolic diseases.

DC260126 is a small-molecule antagonist of FFA1 (GPR40)

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

AMG 837 calcium hydrate is a potent GPR40 agonist with an EC50 of 13 nM. AMG 837 calcium hydrate also shows highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM).

AM-6226 is a potent and orally bioavailable GPR40 full agonist.

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.

DS-1558 is a potent and orally available GPR40 agonist.DS-1558 was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF rats. DS-1558 significantly and dose-dependently improved hyperglycemia and increased insulin secretion during the oral glucose tolerance test in Zucker fatty rats, the model of insulin resistance and glucose intolerance. DS-1558 not only increased the glucose-stimulated insulin secretion by GLP-1 but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats.

AS2575959 is a novel GPR40 agonist, exhibiting glucose metabolism improvement and synergistic effect with sitagliptin on insulin and incretin secretion.

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.

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

LY2922083 is a Potent and Selective GPR40 agonist. LY2922083 demonstrates potent, efficacious and durable dose dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion.

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

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

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

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

AM-5262 is a potent GPR40 Full Agonist with improved rat PK profile and general selectivity profile.

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.