Biological Activity
Novel, potent and selective antagonist of NR2B-containing NMDA receptors (IC50 values are 0.043, > 100 and > 100 μM for NR1A/2B, NR1A/2A and NR1A/2C subunit combinations respectively). Displays neuroprotective effects in vivo and in vitro.
Compound Libraries
Co 101244 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 377.91 |
| Formula | C21H27NO3.HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 193356-17-1 |
| PubChem ID | 6918426 |
| InChI Key | WFFZHKKSIDENAJ-UHFFFAOYSA-N |
| Smiles | Cl.CC1=CC=C(CC2(O)CCN(CCOC3=CC=C(O)C=C3)CC2)C=C1 |
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 | 18.9 | 50 | |
| water | 37.79 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 377.91. 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 | 2.65 mL | 13.23 mL | 26.46 mL |
| 5 mM | 0.53 mL | 2.65 mL | 5.29 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.65 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zhou et al (1999) 4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist. J.Med.Chem. 42 2993 PMID: 10425109
Gill et al (2002) Pharmacological characterization of Ro 63-1908 (1-[2-(4-hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a novel subtype-selective N-methyl-D-aspartate antagonist. J.Pharmacol.Exp.Ther. 302 940 PMID: 12183650
Higgins et al (2003) Evaluation of the NR2B-selective NMDA receptor antagonist Ro 63-1908 on rodent behaviour: evidence for an involvement of NR2B NMDA receptors in response inhibition. Neuropharmacology 44 324 PMID: 12604092
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