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Submit ReviewCo 101244 hydrochloride
Description: GluN2B-selective NMDA antagonist
Alternative Names: PD 174494,Ro 63-1908
Chemical Name: 1-[2-(4-Hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]-4-piperidinol hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for Co 101244 hydrochloride
Co 101244 hydrochloride is a novel, potent and selective antagonist of GluN2B (formally NR2B)-containing NMDA receptors (IC50 values are 0.043, > 100 and > 100 μM for GluN1A/2B (NR1A/2B), GluN1A/2A (NR1A/2A) and GluN1A/2C (NR1A/2C) subunit combinations respectively). Displays neuroprotective effects in vivo and in vitro.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Compound Libraries for Co 101244 hydrochloride
Co 101244 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Co 101244 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Co 101244 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 37.79 | 100 | |
| DMSO | 18.9 | 50 |
Preparing Stock Solutions for Co 101244 hydrochloride
The following data is based on the product molecular weight 377.91. Batch specific molecular weights may vary from batch to batch due to the degree 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 for Co 101244 hydrochloride
References for Co 101244 hydrochloride
References are publications that support the biological activity of the product.
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-MthD.-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
If you know of a relevant reference for Co 101244 hydrochloride, please let us know.
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Keywords: Co 101244 hydrochloride, Co 101244 hydrochloride supplier, selective, NR2B, antagonists, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, Co101244, hydrochloride, PD174494, Ro63-1908, GluN2B, PD, 174494, Ro, 63-1908, 2456, Tocris Bioscience
3 Citations for Co 101244 hydrochloride
Citations are publications that use Tocris products. Selected citations for Co 101244 hydrochloride include:
Mirante et al (2014) Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala. Am J Physiol Renal Physiol 7 62 PMID: 25071439
Peng et al (2008) TRPV1 mediates the uterine capsaicin-induced NMDA NR2B-dependent cross-organ reflex sensitization in anesthetized rats. Neuroscience 295 F1324 PMID: 18632800
Quillinan et al (2015) Region-specific role for GluN2B-containing NMDA receptors in injury to Purkinje cells and CA1 neurons following global cerebral ischemia. J Cell Biol 284 555 PMID: 25450957
Do you know of a great paper that uses Co 101244 hydrochloride from Tocris? Please let us know.
Reviews for Co 101244 hydrochloride
Average Rating: 5 (Based on 1 Review.)
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Impact of Co-101244 on current transfer through neutrophil cell membrane.
By
Sergiy Sylantyev on 07/13/2023
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Blood
Co-101244 was used to quantify the input of GluN2B-containing NMDA receptors into electrical current flow through the membrane of human neutrophil. Figure; normalized electrical response of a single neutrophil after application of Co-101244 (bar +Co).
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