Biological Activity
Potent and selective 5-HT4 receptor antagonist (Ki = 0.19 nM for porcine 5-HT4). Centrally active following systemic administration in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
| M. Wt | 524.58 |
| Formula | C19H26FN3O5S.H2NSO3H |
| Storage | Desiccate at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 859502-43-5 |
| PubChem ID | 6604955 |
| InChI Key | VQJFDBXITIOGJM-UHFFFAOYSA-N |
| Smiles | NS(O)(=O)=O.COC1=C(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)C2=CC(F)=CC=C2N1 |
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 | |||
| phosphate buffered saline | 2.14 | 5mM with gentle warming | |
| water | 4.27 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 524.58. 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 | 1.91 mL | 9.53 mL | 19.06 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.81 mL |
| 10 mM | 0.19 mL | 0.95 mL | 1.91 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Galeotti et al (1998) Role of 5-HT4 receptors in the mouse passive avoidance test. J.Pharmacol.Exp.Ther. 286 1115 PMID: 9732367
Horikoshi et al (2001) Possible involvement of 5-HT4 receptors, in addition to 5-HT3 receptors, in the emesis induced by high-dose cisplatin in Suncus murinus. Jpn.J.Pharmacol. 85 70 PMID: 11243577
Schiavi et al (1994) Identification of serotonin 5-HT4 recognition sites in the porcine caudate nucleus by radioligand binding. Neuropharmacology 33 543 PMID: 7984293
Keywords: GR 125487 sulfamate, supplier, Potent, selective, 5-HT4, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, GR125487, sulfamate, GlaxoSmithKline, GSK, 5-HT4, Receptors, 5-HT4, Receptors, Tocris Bioscience
