Biological Activity
Potent, selective 5-HT4 receptor antagonist (pKB = 9.43 in human colonic muscle, and Kd = 0.15 nM for binding to cloned human 5-HT4 receptors). Displays > 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
Licensing Information
Sold with the permission of GlaxoSmithKline
Technical Data
| M. Wt | 393.5 |
| Formula | C19H27N3O4S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 144625-51-4 |
| PubChem ID | 5730 |
| InChI Key | PYEFPDQFAZNXLI-UHFFFAOYSA-N |
| Smiles | CN1C=C(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)C2=CC=CC=C12 |
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 | |||
| 1eq. HCl | 9.84 | 25 | |
| DMSO | 4.72 | 12 | |
| ethanol | 19.68 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 393.5. 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 | 2.54 mL | 12.71 mL | 25.41 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.08 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.54 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Eglen et al (1995) Central 5-HT4 receptors. TiPS 16 391 PMID: 8578609
Gale et al (1994) GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. Br.J.Pharmacol. 111 332 PMID: 8012715
Prins et al (2000) An improved in vitro bioassay for the study of 5-HT4 receptors in the human isolated large intestinal circular muscle. Br.J.Pharmacol. 129 1601 PMID: 10780964
Van den Wyngaert et al (1997) Cloning and expression of a human serotonin 5-HT4 receptor cDNA. J.Neurochem. 69 1810 PMID: 9349523
Keywords: GR 113808, supplier, Potent, selective, 5-HT4, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, GR113808, GlaxoSmithKline, GSK, 5-HT4, Receptors, 5-HT4, Receptors, Tocris Bioscience
