SB 271046 hydrochloride

Name: SB 271046 hydrochloride
Brand: Tocris Bioscience
SKU: 3368

Tocris Bioscience, part of Bio-Techne | Catalog # 3368

Citations (6)

COA / SDS

Selective 5-HT6 antagonist; orally active

Key Product Details

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:	≥98% (HPLC)
Molecular Weight:	488.45

View Full Technical Details for SB 271046 hydrochloride

Technical Data
Citations

Biological Activity for SB 271046 hydrochloride

SB 271046 hydrochloride is a selective, orally active 5-HT₆ antagonist (pK_i 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-HT_1D, 5-HT_1A, D₃, 5-HT_1B, 5-HT_1F, α_1B, 5-HT_2C, 5-HT_2A, D₂, 5-HT_2B, 5-HT₇, 5-HT₄ and 5-HT_1E 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 for SB 271046 hydrochloride

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 for SB 271046 hydrochloride

M. Wt	488.45
Formula	C₂₀H₂₂ClN₃O₃S₂.HCl
Storage	Desiccate at RT
Purity	≥98% (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 for SB 271046 hydrochloride

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

Preparing Stock Solutions for SB 271046 hydrochloride

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.

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	0.20 mL	1.02 mL	2.05 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

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References for SB 271046 hydrochloride

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

Marcos Effects of 5-HT₆ receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br.J.Pharmacol. 2008 PMID: 18622410
Dawson 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. 2000 PMID: 10780993
Routledge Characterization of SB-271046: a potent, selective and orally active 5-HT₆ receptor antagonist. Br.J.Pharmacol. 2000 PMID: 10928964
Bromidge 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. 1999 PMID: 9925723