<p>A series of novel dual-action statin conjugates, which exhibit both triglyceride and cholesterol lowering activities, have been systematically designed, synthesized, and subjected to comprehensive pharmacological evaluation. All the target compounds were characterized by ¹HNMR, ¹³CNMR, and HRMS. Biological evaluation demonstrated that the majority of the synthesized compounds exhibited significant lipid-lowering and cholesterol-reducing activities. In particular, ligand 8a demonstrated significant potency, resulting in a marked reduction in cholesterol and triglyceride levels in a dose-dependent manner. Its minimum response has lowered 2.778&#xa0;mmol/L (cholesterol level) and 0.699&#xa0;mmol/L (triglycerides level), surpassing the positive control. For the preliminary assessment of the safety of the target compound, the ADMETlab 2.0 predictive software was utilized. Data show that compared to the combination of drugs used clinically, the safety of the target compounds may be improved. These findings suggest that compound 8a holds promise as a potential candidate for the treatment of hyperlipidemia.</p>