RAGE/SERT-IN-1 is a potent, orally active inhibitor of advanced glycation end products (RAGE) and serotonin transporter (SERT), with IC50 values of 8.26 μM and 31.09 nM, respectively. It demonstrates a significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior in mice. RAGE/SERT-IN-1 is useful for research on the comorbidity of Alzheimer's disease and depression [1].

RAGE/SERT-IN-1（化合物12）（1-20 μM；24小时）对SH-SY5Y细胞[1]的存活率没有显著影响。

RAGE/SERT-IN-1 (0-10 μM; 60分钟) 在肝微粒体中展现出良好的稳定性，且未明显抑制主要CYP酶[1]。RAGE/SERT-IN-1（100和200mg/kg; 腹腔注射; 单次剂量）未引起小鼠死亡，且在100 mg/kg剂量下器官与体重比率无显著变化[1]。RAGE/SERT-IN-1（60 mg/kg; 口服; 单次剂量）显著降低小鼠尾悬挂实验中的不动时间[1]。RAGE/SERT-IN-1（口服60 mg/kg，静脉注射10 mg/kg; 单次剂量）在小鼠中表现出可接受的药代动力学特性[1]。雄性ICR小鼠RAGE/SERT-IN-1的药代动力学参数[1]包括口服（60 mg/kg）和静脉注射（10 mg/kg）的T 1/2（小时）分别为5.55和3.46，C max（ng/mL）分别为4935和51745，AUC 0-∞（ng/mL·h）分别为24684和23653，CL（mL/min/kg）为7.09，V SS（L/kg）为1037，F（%）为17.1。