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2766739-35-7
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RAGE/SERT-IN-1
CAS No. : 2766739-35-7
MCE 国际站：RAGE/SERT-IN-1
产品活性：RAGE/SERT-IN-1 是一种有效且具有口服活性的晚期糖基化终产物 (RAGE) 和 血清素转运蛋白 (SERT) 抑制剂，IC50 分别为 8.26 μM 和 31.09 nM。RAGE/SERT-IN-1 对 Aβ25-35 诱导的神经元损伤具有显著的神经保护作用，能减轻小鼠的抑郁行为。RAGE/SERT-IN-1 可用于研究阿尔茨海默病和抑郁症的合并症。
研究领域：Neuronal Signaling
作用靶点：Amyloid-β | Serotonin Transporter
In Vitro: RAGE/SERT-IN-1 (compound 12) (1-20 μM; 24 hours) does not significantly affect cell viability of SH-SY5Y.
In Vivo: RAGE/SERT-IN-1 (0-10 μM; 60 min) has good liver microsomal stability and does not apparently inhibit main CYP enzymes.
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.
RAGE/SERT-IN-1 (60 mg/kg; PO; single dosage) significantly reduces the immobility time in tail suspension test.
RAGE/SERT-IN-1 (60 mg/kg for PO, 10 mg/kg for IV; single dosage) exhibits acceptable pharmacokinetic properties in mice.
Pharmacokinetic Parameters of RAGE/SERT-IN-1 in male ICR mice.
| PO (60 mg/kg) | IV (10 mg/kg) | |
| T1/2 (h) | 5.55 | 3.46 |
| Cmax (ng/mL) | 4935 | 51745 |
| AUC0-∞ (ng/mL·h) | 24684 | 23653 |
| CL (mL/min/kg) | 7.09 | |
| VSS (L/kg) | 1037 | |
| F (%) | 17.1 |
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