BMS-986118

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^{[1][2][3][4][5][6][7]}. IC50 & Target:IC₅₀: 0.07 µM (GPR40)^[1] In Vitro:BMS-986118 exhibits potent hGPR40 agonist activity with an EC₅₀ of 0.07 μM^[1].
BMS-986118 (<10 μM) is highly selective and shows no significant activity against a broad panel of off-target targets at concentrations up to 10 μM^[1].
BMS-986118 is a highly selective and potent full agonist of GPR40, exhibiting an hEC₅₀ of 70 nM in the GPR40 CHO cell line^[3].
BMS-986118 acts as a full FFA1 agonist in vitro, stimulating GSIS in Min6 cells and GLP-1 secretion in STC1 cells^[6].
BMS-986118 acts as a full agonist to enhance insulin secretion in MIN6 cells and GLP-1 secretion in STC1 cells^[5]. In Vivo:BMS-986118 (0.03-1 mg/kg; p.o.; single dose) dose-dependently suppresses plasma glucose excursions in mice during the IPGTT, with glucose-lowering effects observed at 0.1 mg/kg^[1].
BMS-986118 (3 mg/kg; single dose), when combined with a DPP4 inhibitor, enhances glucose-stimulated insulin secretion and promotes GLP-1 secretion in mice, demonstrating a dual mechanism of action^[1].
BMS-986118 (1-15 mg/kg; p.o.) exhibits in vivo efficacy in the ZDF type 2 diabetic rat model by increasing GLP-1 secretion and reducing HbA_1c levels^[6].