RS 39604 hydrochloride

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Cat.No. 0991 - RS 39604 hydrochloride | C26H36ClN3O6S.HCl | CAS No. 167710-87-4
Description: 5-HT4 antagonist
Chemical Name: 1-[4-Amino-5-chloro-2-(3,5-dimethoxyphenyl)methyloxy]-3-[1-[2-methylsulphonylamino]ethyl]piperidin-4-yl]propan-1-one hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews
Literature (4)

Biological Activity

A potent and selective 5-HT4 antagonist, with a pKi of 9.1 at 5-HT4 receptors in guinea pig striatal membranes and greater than 1000-fold selectivity over 5-HT1A, 2C, 3 and D1, D2, M1, M2, AT1, B1 and α1C receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo studies.

Licensing Information

Sold with the permission of Roche Bioscience

Compound Libraries

RS 39604 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 590.56
Formula C26H36ClN3O6S.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 167710-87-4
PubChem ID 19081934
InChI Key QSMYZGMJSGUWPM-UHFFFAOYSA-N
Smiles Cl.COC1=CC(OC)=CC(COC2=CC(N)=C(Cl)C=C2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)=C1

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 59.06 100

Preparing Stock Solutions

The following data is based on the product molecular weight 590.56. 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 1.69 mL 8.47 mL 16.93 mL
5 mM 0.34 mL 1.69 mL 3.39 mL
10 mM 0.17 mL 0.85 mL 1.69 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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References

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

Eglen et al (1995) Central 5-HT4 receptors TiPS 16 391 PMID: 8578609

Hegde (1995) RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist. Br.J.Pharmacol. 115 1087 PMID: 7582507


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3 Citations for RS 39604 hydrochloride

Citations are publications that use Tocris products. Selected citations for RS 39604 hydrochloride include:

Ratner et al (2012) Cerebral markers of the serotonergic system in rat models of obesity and after Roux-en-Y gastric bypass. Learn Mem 20 2133 PMID: 22450706

Müller et al (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One 4 e6453 PMID: 19649285

Huang and Kandel (2007) Low-frequency stimulation induces a pathway-specific late phase of LTP in the amygdala that is mediated by PKA and dependent on protein synthesis. J Pharmacol Exp Ther 14 497 PMID: 17626908


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Literature in this Area

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