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Tocris/SB 271046 hydrochloride/3368/50/50 mg

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货号: 3368/50

品牌: Tocris

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Description: Selective, orally active 5-HT₆ antagonist

Chemical Name: 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophen-2-sulfonamide hydrochloride

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

SB 271046 hydrochloride is also offered as part of the Tocriscreen Plus. 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 solvent 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	0.2 mL	1.02 mL	2.05 mL
50 mM	0.04 mL	0.2 mL	0.41 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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, dopamine, 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

Keywords: SB 271046 hydrochloride, supplier, Orally, active, selective, 5-HT6, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB271046, hydrochloride, GlaxoSmithKline, GSK, 5-HT6, Receptors, 5-HT6, Receptors, Tocris Bioscience

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