1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 5HT6-ligand-1

5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM.

For research use only. We do not sell to patients.

5HT6-ligand-1 Chemical Structure

5HT6-ligand-1 Chemical Structure

CAS No. : 1038988-11-2

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Description

5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM.

IC50 & Target

5-HT6 Receptor

1.43 nM (Ki)

In Vivo

5HT6-ligand-1 is extensively metabolized in rat liver microsomes whereas in human liver microsomes, 5HT6-ligand-1 is extensively metabolized (90%). The IC50 values for 5HT6-ligand-1 at CYP 3A4 is 35.97%, whereas the IC50 values at CYP 2D6 enzymes is less than 20 μM. 5HT6-ligand-1 at an oral dose of 10 mg/kg is rapidly absorbed in rats with a good oral half-life of 3.17±0.49 h with an oral bioavailability of 29±5%. The observed oral Cmax is 60±44 ng/mL and occurs at 1.83 h. 5HT6-ligand-1 displays an oral exposure of 217±92 ng h/mL. It has a clearance of 220±92 mL/min/kg with a volume of distribution of 32.6±10.7 L/kg for iv dose. Extensive rat metabolism coupled with high clearance could be the possible reason for moderate oral bioavailability showed by 5HT6-ligand-1. Oral administration of 5HT6-ligand-1 reverses the time delay induced memory deficit and statistically significant effect is observed at a dose of 10 mg/kg indicating cognitive improvement potential of the compound 6a[1].

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

Molecular Weight

448.38

Formula

C20H22BrN3O2S

CAS No.
SMILES

CN1CCN(CC2=CC=CC3=C2C=CN3S(=O)(C4=CC=CC=C4Br)=O)CC1

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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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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.

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5HT6-ligand-1
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HY-U00126
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