| Bioactivity | RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression[1]. |
| Target | IC50: 8.26 μM (RAGE), 31.09 nM (SERT) |
| Invitro | RAGE/SERT-IN-1 (compound 12) (1-20 μM; 24 hours) does not significantly affect cell viability of SH-SY5Y[1]. Cell Cytotoxicity Assay Cell Line: |
| In Vivo | RAGE/SERT-IN-1 (0-10 μM; 60 min) has good liver microsomal stability and does not apparently inhibit main CYP enzymes[1].RAGE/SERT-IN-1 (100 and 200mg/kg; IP; single dosage) does not cause mice death and not significant change in the ratio of organ-to-body weight at 100 mg/kg[1].RAGE/SERT-IN-1 (60 mg/kg; PO; single dosage) significantly reduces the immobility time in tail suspension test[1].RAGE/SERT-IN-1 (60 mg/kg for PO, 10 mg/kg for IV; single dosage) exhibits acceptable pharmacokinetic properties in mice[1].Pharmacokinetic Parameters of RAGE/SERT-IN-1 in male ICR mice[1]. |
| Name | RAGE/SERT-IN-1 |
| Formula | C38H41ClN4OS |
| Molar Mass | 637.28 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhang C, Wang L, Xu Y, et al. Discovery of novel dual RAGE/SERT inhibitors for the potential treatment of the comorbidity of Alzheimer's disease and depression. Eur J Med Chem. 2022;236:114347. |