Biological Activity
High affinity 5-HT2B receptor antagonist (pKi = 9.5). Displays 1000-fold selectivity for 5-HT2B with good bioavailability.
Technical Data
| M. Wt | 317.79 |
| Formula | C17H16FN3.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 199864-86-3 |
| PubChem ID | 9905058 |
| InChI Key | MKJPYBJBPRFMHL-UHFFFAOYSA-N |
| Smiles | FC1=C(C=CC=C2)C2=C(C3=CC(C(C)C)=NC(N)=N3)C=C1.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 | |||
| DMSO | 31.78 | 100 | |
| ethanol | 31.78 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 317.79. 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 | 3.15 mL | 15.73 mL | 31.47 mL |
| 5 mM | 0.63 mL | 3.15 mL | 6.29 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.15 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bonhaus et al (1999) RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br.J.Pharmacol. 127 1075 PMID: 10455251
Callebert et al (2006) Evidence for a control of plasma serotonin levels by 5-Hydroxytryptamine2B receptors in mice. J.Pharmacol.Exp.Ther. 317 724 PMID: 16461587
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