GPR109 receptor agonist-3 is an orally active GPR109 receptor agonist with an IC50 of 310 nM. It retains the antioxidant and cytoprotective properties of lipoic acid. In rats on a high-fat diet, GPR109 receptor agonist-3 reduces total cholesterol (TC), triglycerides (TG), and low-density lipoprotein cholesterol (LDL-C), while increasing high-density lipoprotein cholesterol (HDL-C). This compound is applicable for atherosclerosis research.

GPR109 receptor agonist-3 (Compound N2L) (10-100 μM, pretreated for 30 minutes) significantly reduces L-glutamate-induced toxicity in HT22 cells and effectively decreases H2O2-induced toxicity in HUVECs, thereby improving cell viability.

GPR109 receptor agonist-3 (Compound N2L), administered orally at 60 mg/kg once daily for four weeks, reduces total cholesterol (TC), triglycerides (TG), and low-density lipoprotein cholesterol (LDL-C) while increasing high-density lipoprotein cholesterol (HDL-C) in rats on a high-fat diet. Furthermore, when included in the diet at 0.03%-0.1% and administered orally for nine weeks, it decreases aortic plaque area and lowers serum levels of TC, TG, and LDL-C in ApoE knockout mice. It also raises HDL-C levels, reduces vascular superoxide production, decreases liver malondialdehyde (MDA) levels, and inhibits weight gain.