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

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.

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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 Related Antibodies

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Description

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]
In Vitro

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

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

RAGE/SERT-IN-1 Related Antibodies

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%.
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

MedChemExpress (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.
Molecular Weight

637.28

Formula

C38H41ClN4OS
CAS No.
SMILES

CCCCC1=C(N=C(S1)C2CCN(CC2)CCCCC3=CN(C4=C3C=C(C=C4)C#N)C)C5=CC=C(C=C5)OC6=CC=C(C=C6)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RAGE/SERT-IN-1 Related Classifications

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× = ×
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Help & FAQs
  • 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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