Biological Activity
Highly potent NR2B-selective NMDA receptor antagonist (Ki = 0.8 nM); blocks NR2B-mediated calcium influx in Ltk cells (Ki = 9.7 nM). Selective for NR2B subunit over α1-adrenergic receptors and hERG channels (IC50 values are 730 nM and 2900 nM respectively). Displays efficacy in the rat carrageenan-induced mechanical hyperalgesia assay.
Technical Data
| M. Wt | 412.33 |
| Formula | C20H22FN3O.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 700878-19-9 |
| PubChem ID | 90488908 |
| InChI Key | JYUWGWCFJMDMND-UHFFFAOYSA-N |
| Smiles | FC1=CC=CC=C1CC(CC4)CCN4CC3=NC2=CC=C(O)C=C2N3.Cl.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 | |||
| water | 41.23 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 412.33. 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 | 2.43 mL | 12.13 mL | 24.25 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.85 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.43 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
McCauley et al (2004) NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. J.Med.Chem. 47 2089 PMID: 15056006
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