ffa1

FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor (FFA1) agonist (EC50: 0.75 μM).

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.

GSK137647A (GSK 137647) is a selective FFA4 agonist.

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

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)

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

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.

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

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.

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.

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).

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

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).

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

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.

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

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

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

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