2. Neuronal Signaling
  3. Amyloid-β Serotonin Transporter
  4. RAGE/SERT-IN-1

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。

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RAGE/SERT-IN-1 Chemical Structure

RAGE/SERT-IN-1 Chemical Structure

CAS No. : 2766739-35-7

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RAGE/SERT-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

IC50: 8.26 μM (RAGE), 31.09 nM (SERT)[1]
体外研究
(In Vitro)

RAGE/SERT-IN-1 (compound 12) (1-20 μM; 24 hours) does not significantly affect cell viability of SH-SY5Y[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RAGE/SERT-IN-1 相关抗体:

Cell Cytotoxicity Assay

Cell Line: SH-SY5Y[1]
Concentration: 1, 5, 10 and 20 μM
Incubation Time: 24 hours
Result: Did not affect cell viability at concentrations of 1, 5, and 10 μM, and only a slight decrease in cell viability at the concentration of 20 μM was observed with the viability still above 80%.
体内研究
(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].

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (24-26 g)[1]
Dosage: 100mg/kg and 200mg/kg
Administration: IP; single (observed for 2 weeks)
Result: All mice were survived and no significant changed in the ratio of organ-to-body weight at a dose of 100 mg/kg.
Animal Model: Male ICR mice[1]
Dosage: 60 mg/kg
Administration: PO; single dosage
Result: Significantly reduced the immobility time in tail suspension test.
Animal Model: Male ICR mice[1]
Dosage: 60 mg/kg for PO, 10 mg/kg for IV
Administration: PO and IV; single dosage
Result: Exhibited acceptable pharmacokinetic properties in mice.
分子量

637.28

Formula

C38H41ClN4OS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RAGE/SERT-IN-1 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RAGE/SERT-IN-12766739-35-7Amyloid-βSerotonin Transporterβ-amyloid peptideAβAbeta5-HTTSERTSLC6A4NeuroprotectiveAlzheimer's diseaseDepressionICR miceOrally activeInhibitorinhibitorinhibit

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