gpr40/ffar1

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

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.

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

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

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 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].

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

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.