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.
For research use only. We do not sell to patients.
- CAS No.: 2766739-35-7
- Formula: C38H41ClN4OS
- Molecular Weight:637.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:SH-SY5Y[1]
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Concentration:1, 5, 10 and 20 μM
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Incubation Time:24 hours
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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 (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.
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Animal Model:Male ICR mice (24-26 g)[1]
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Dosage:100mg/kg and 200mg/kg
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Administration:IP; single (observed for 2 weeks)
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Result:All mice were survived and no significant changed in the ratio of organ-to-body weight at a dose of 100 mg/kg.
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Animal Model:Male ICR mice[1]
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Dosage:60 mg/kg
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Administration:PO; single dosage
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Result:Significantly reduced the immobility time in tail suspension test.
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Animal Model:Male ICR mice[1]
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Dosage:60 mg/kg for PO, 10 mg/kg for IV
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Administration:PO and IV; single dosage
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Result:Exhibited acceptable pharmacokinetic properties in mice.
Chemical Information
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CAS No. 2766739-35-7
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Molecular Weight 637.28
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Formula C38H41ClN4OS
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RAGE/SERT-IN-1 Related Classifications
HY-146619 Related Classifications
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