2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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.

5HT6-ligand-2 Chemical Structure

5HT6-ligand-2 Chemical Structure

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5HT6-ligand-2 Related Antibodies

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Description

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[1].

IC50 & Target[1]

5-HT6 Receptor

 

In Vivo

BET-IN-26 (compound 13a) (10, 100 mg/kg; p.o.) decreases the LPS (HY-D1056) induced serum levels of IL-6 and MCP-1 in a dose-dependent manner in mice[1].
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.

Animal Model: 230-260 g, 8 weeks old Male Wistar rats (MK-801-induced memory impairment)[1]
Dosage: 2.5, 5, 7.5 mg/kg
Administration: I.p.; 30 min before testing
Result: Significantly reduced immobility time by 30.5 % and increased climbing behaviors by 63 %, without affecting the duration of swimming at 5 mg/kg.
Molecular Weight

476.57

Formula

C29H28N6O
SMILES

O=C1N(CC2=CC=CC=C2)C3=CC=CC(N(CC4)CCN4CCC5=CNC6=C5C=C(C#N)C=C6)=C3N1
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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5HT6-ligand-2 Related Classifications

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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:

5HT6-ligand-25-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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