FFAR1 Agonist

MK-2305 is an orally active GPR40 partial agonist with an EC₅₀ of 6 nM in rats. MK-2305 mediates glucose-stimulated insulin secretion and inhibits endogenous glucose production by reducing gluconeogenesis from tricarboxylic acid (TCA) cycle substrates. MK-2305 increases plasma insulin levels under hyperglycemic and glucose-stimulated conditions, reduces fasting blood glucose, and improves glucose homeostasis. MK-2305 can be used in studies related to type 2 diabetes.

Xelaglifam is an orally active GPR40/FFAR1 agonist and PPARγ coactivator recruitment inhibitor (IC₅₀ 74.7 µM). Xelaglifam activates Gq/IP3/Ca²⁺ and β-arrestin, stimulates glucose-dependent insulin secretion from pancreatic β cells, improves glucose tolerance, reduces fasting hyperglycemia, protects pancreatic β cells, inhibits DP1, BSEP (IC₅₀ 14.3 µM), MRP2 (39.9 µM) and MRP4 (4.4 µM), activates FXR, regulates bile acid homeostasis, and modulates mitochondrial function, membrane potential and cellular ATP. Xelaglifam can be used for research on type 2 diabetes.

BMS-986118 is an orally active and selective GPR40 full agonist (EC₅₀ = 0.07 μM). BMS-986118 induces GLP-1 secretion and increases GLP-1 and insulin levels when combined with DPP-4 inhibitors. BMS-986118 shows sustained glucose-lowering effects. BMS-986118 can be used for research on type 2 diabetes.