GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9. GW1100 acts as a GPR40 inverse agonist.
AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor[1].
GPR40 agonist 6 (Compound 7a) is a potent and selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist with an EC50 of 0.058 μM[1].
FFA3 agonist 1 (Compound 24) is an agonist of free fatty acid receptor 3 (FFA3). FFA3 agonist 1 regulates the health effect of intestinal microbiota by activating FFA3[1].
PBI-4050 acts as an agonist for GPR40 and as an antagonist or inverse agonist for GPR84.
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM)[1].
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.IC50 value:Target: GPR40Preparation of spiropiperidine derivatives for use as antidiabetic agentsBy Hamdouchi, Chafiq; Lineswala, Jayana Pankaj; Maiti, Pranab From PCT Int. Appl. (2011), WO 2011066183 A1 20110603.
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120[1][2].
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.IC50 value: 7.32 (pEC50) [1]Target: GPR40GW9508 is shown to be at least 100-fold selective against 220 other GPCRs, 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ (pEC50 4.0, 4 and 4.9, respectively). GW9508 produces a concentration-dependent increase in intracellular Ca2+ concentrations via GPR40 receptor activation and the GPR120 receptor. GW9508 is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. GW9508 produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). GW9508 dose dependently stimulated insulin secretion in a glucose-sensitive manner in MIN6 cells. Furthermore, GW9508 is able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. [1] GW9508 induced hyperpolarization and opening of KATP channels in rat β-cells. [2] GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes. [3]
AM-4668 is a GPR40 agonist for type 2 diabetes. EC50s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively[1].
BTI-A-404 is a potent, selective and competitive inverse agonist of human GPR43. BTI-A-404 can be used for the research of inflammation, obesity and type 2 diabetes[1].