5HT6-ligand-1


Catalog No. Size PriceQuantity
M21820-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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

Product information

CAS Number: 1038988-11-2

Molecular Weight: 448.38

Formula: C20H22BrN3O2S

Chemical Name: 1-(2-bromobenzenesulfonyl)-4-[(4-methylpiperazin-1-yl)methyl]-1H-indole

Smiles: CN1CCN(CC2=CC=CC3=C2C=CN3S(=O)(=O)C2=CC=CC=C2Br)CC1

InChiKey: AGKMPGSBLMAGAX-UHFFFAOYSA-N

InChi: InChI=1S/C20H22BrN3O2S/c1-22-11-13-23(14-12-22)15-16-5-4-7-19-17(16)9-10-24(19)27(25,26)20-8-3-2-6-18(20)21/h2-10H,11-15H2,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.

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