5HT6-ligand-2
5HT6-ligand-2 (compound 15) is a potent 5-HT6 inhibitor with Ki values of 3.4, 15 nM for 5-HT6, SERT, respectively. 5HT6-ligand-2 shows neuroprotection. 5HT6-ligand-2 has the potential for the research of dementia.
For research use only. We do not sell to patients.
- Formula: C29H28N6O
- Molecular Weight:476.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT6 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
83 μM
Compound: 15
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Hepatotoxicity in human HepG2 cells incubated for 24 hrs by PrestoBlue reagent based assay
Hepatotoxicity in human HepG2 cells incubated for 24 hrs by PrestoBlue reagent based assay
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[PMID: 38901106] |
| HT-22 | IC50 |
>100 μM
Compound: 15
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Neurotoxicity in mouse HT-22 cells incubated for 24 hrs by PrestoBlue reagent based assay
Neurotoxicity in mouse HT-22 cells incubated for 24 hrs by PrestoBlue reagent based assay
|
[PMID: 38901106] |
Pharmacokinetic Parameters (2.5 mg/kg; i.p.; Male Wistar rats)[1].
| Parameter | Serum | Brain |
| Cmax (ng/ml(g)) | 45.21 | 3.78 |
| tmax (min) | 30 | 30 |
| lz (min-1) | 0.0099 | 0.0072 |
| t0.5 (min) | 70.08 | 96.71 |
| Vz/F (l/kg) | 55.87 | - |
| CL/F (l/min/kg) | 0.55 | - |
| AUC(0-inf) (ng/mL*min) | 4542.15 | 606.48 |
| MRT (min) | 104.27 | 152.35 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:230-260 g, 8 weeks old Male Wistar rats (MK-801-induced memory impairment)[1]
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Dosage:2.5, 5, 7.5 mg/kg
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Administration:I.p.; 30 min before testing
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Result:Significantly reduced immobility time by 30.5 % and increased climbing behaviors by 63 %, without affecting the duration of swimming at 5 mg/kg.
Chemical Information
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Molecular Weight 476.57
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Formula C29H28N6O
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SMILES
O=C1N(CC2=CC=CC=C2)C3=CC=CC(N(CC4)CCN4CCC5=CNC6=C5C=C(C#N)C=C6)=C3N1
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)