SB 258719 hydrochloride

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Cat.No. 2726 - SB 258719 hydrochloride | C18H30N2O2S.HCl | CAS No. 1217674-10-6
Description: Selective 5-HT7 antagonist
Chemical Name: 3-Methyl-N-[(1R)-1-methyl-3-(4-methyl-1-piperidinyl)propyl]-N-methylbenzenesulfonamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Reviews
Literature (4)

Biological Activity

Selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries

SB 258719 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 374.97
Formula C18H30N2O2S.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 1217674-10-6
PubChem ID 56972181
InChI Key UIZKHTBWJSUGOV-UNTBIKODSA-N
Smiles O=S(C1=CC(C)=CC=C1)(N(C)[C@H](C)CCN2CCC(C)CC2)=O.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
water 37.5 100
DMSO 37.5 100

Preparing Stock Solutions

The following data is based on the product molecular weight 374.97. 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 2.67 mL 13.33 mL 26.67 mL
5 mM 0.53 mL 2.67 mL 5.33 mL
10 mM 0.27 mL 1.33 mL 2.67 mL
50 mM 0.05 mL 0.27 mL 0.53 mL

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References

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

Forbes et al (1998) (R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl)propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist. J.Med.Chem. 41 655 PMID: 9513592

Thomas et al (1998) Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br.J.Pharmacol. 124 1300 PMID: 9720804

Guscott et al (2003) The hypothermic effect of 5-CT in mice is mediated through the 5-HT7receptor. Neuropharmacology 44 1031 PMID: 12763096


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Keywords: SB 258719 hydrochloride, SB 258719 hydrochloride supplier, Selective, 5-HT7, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB258719, hydrochloride, GlaxoSmithKline, GSK, 2726, Tocris Bioscience

3 Citations for SB 258719 hydrochloride

Citations are publications that use Tocris products. Selected citations for SB 258719 hydrochloride include:

Johnson et al (2011) Serotonin receptor activity is necessary for olfactory learning and memory in Drosophila melanogaster. Neuroscience 192 372 PMID: 21749913

Zhao et al (2015) Fisetin exerts antihyperalgesic effect in a mouse model of neuropathic pain: engagement of spinal serotonergic system. Front Synaptic Neurosci 5 9043 PMID: 25761874

Domínguez-Soto (2017) Serotonin drives the acquisition of a profibrotic and anti-inflammatory gene profile through the 5-HT7R-PKA signaling axis. Sci Rep 7 14761 PMID: 29116249


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Literature in this Area

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