Co 101244 hydrochloride

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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)
Datasheet
Citations (3)
Reviews (1)
Literature (6)

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.

Select a batch to recalculate based on the batch molecular weight:
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


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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:

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

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


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Reviews for Co 101244 hydrochloride

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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).

Reference
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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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