SB 271046 hydrochloride

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Cat.No. 3368 - SB 271046 hydrochloride | C20H22ClN3O3S2.HCl | CAS No. 209481-24-3
Description: Selective 5-HT6 antagonist; orally active
Chemical Name: 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophen-2-sulfonamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM).

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries

SB 271046 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 488.45
Formula C20H22ClN3O3S2.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 209481-24-3
PubChem ID 6918455
InChI Key RMXZRJYGJMSDQK-UHFFFAOYSA-N
Smiles CC2=C(S(NC3=CC=C(OC)C(N4CCNCC4)=C3)(=O)=O)SC1=CC=C(Cl)C=C12.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 48.84 100

Preparing Stock Solutions

The following data is based on the product molecular weight 488.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.05 mL 10.24 mL 20.47 mL
5 mM 0.41 mL 2.05 mL 4.09 mL
10 mM 0.2 mL 1.02 mL 2.05 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Bromidge et al (1999) 5-Chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzothiophenesulfonamide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J.Med.Chem. 42 202 PMID: 9925723

Dawson et al (2000) In vivo effects of the 5-HT6 antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, DA, 5-HT, glutamate and aspartate. Br.J.Pharmacol. 130 23 PMID: 10780993

Routledge et al (2000) Characterization of SB-271046: a potent, selective and orally active 5-HT6 receptor antagonist. Br.J.Pharmacol. 130 1606 PMID: 10928964

Marcos et al (2008) Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br.J.Pharmacol. 155 434 PMID: 18622410


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