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| Targets |
NR2B subunit of the NMDA receptor. CO-101244 is a potent and selective antagonist of the NR2B-containing NMDA receptors. It has a Ki of approximately 10 nM for the NR2B subunit, with significantly lower affinity for other NMDA receptor subunits. By selectively blocking NR2B-containing receptors, it can modulate glutamatergic signaling.
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| ln Vitro |
Co 101244 enhances neuroprotective effects and significantly decreases the rise in Ca2+ produced by NMDA [1].
CO-101244 potently inhibits NR2B-containing NMDA receptors in vitro. In receptor binding assays, it has a Ki of approximately 10 nM. It shows significant selectivity for NR2B over NR2A and NR2C subunits. In functional assays, it can block NMDA-induced calcium influx and excitotoxicity in neuronal cultures. |
| ln Vivo |
Co 101244 (0.1, 1 mg/kg sc) preserved the motor advantages of levodopa while exhibiting antidyskinetic effects (67% and 71% decrease, respectively) [1].
In vivo, CO-101244 has been studied for its neuroprotective effects in animal models of stroke, traumatic brain injury, and neurodegenerative diseases. It has been shown to reduce infarct size, improve neurological outcomes, and protect against neuronal death. Its selectivity for NR2B may contribute to its neuroprotective effects while reducing the side effects associated with non-selective NMDA antagonists. |
| Enzyme Assay |
In vitro receptor binding assays for CO-101244 involve measuring its affinity for NMDA receptor subunits using radioligand binding techniques. Membranes from cells expressing NR2B or other subunits are incubated with radiolabeled ligands, such as [3H]ifenprodil, and increasing concentrations of CO-101244. Ki values are determined from competition binding curves.
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| Cell Assay |
Cellular assays for CO-101244 involve treating neuronal cells with the compound and measuring NMDA receptor-mediated calcium influx or excitotoxicity. Cells are loaded with calcium-sensitive dyes and stimulated with NMDA in the presence or absence of CO-101244. The compound's ability to block NMDA-induced calcium influx is assessed.
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| Animal Protocol |
In vivo animal studies for CO-101244 typically involve administration to rodent models of stroke, trauma, or neurodegeneration. Efficacy is assessed by measuring infarct size, neurological scores, or neuronal survival. The compound is typically administered intraperitoneally or intravenously. Pharmacokinetic parameters may also be determined.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for CO-101244 is limited. As a research compound, its properties such as bioavailability and half-life are typically characterized in preclinical studies. The compound is generally soluble in DMSO and is formulated for administration via intraperitoneal or intravenous routes.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CO-101244 are limited. As a research tool, its safety profile is primarily assessed in the context of in vivo efficacy studies. The compound's selectivity for NR2B may contribute to a favorable safety profile compared to non-selective NMDA antagonists. Comprehensive toxicological evaluation is needed before any clinical development.
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| References | |
| Additional Infomation |
NMDA receptor NR2B subunit blocker; structure described in the first article.
CO-101244 hydrochloride is a potent and selective antagonist of the NR2B subunit of the NMDA receptor. It has been studied for its potential neuroprotective effects in stroke, traumatic brain injury, and neurodegenerative diseases. Its selectivity for NR2B makes it a valuable tool for studying the role of this subunit in NMDA receptor-mediated processes. |
| Molecular Formula |
C21H27NO3.HCL
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|---|---|
| Molecular Weight |
377.90492
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| Exact Mass |
377.175
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| Elemental Analysis |
C, 66.74; H, 7.47; Cl, 9.38; N, 3.71; O, 12.70
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| CAS # |
193356-17-1
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| Related CAS # |
193359-26-1;193356-17-1 (HCl);
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| PubChem CID |
6918426
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)CC2(CCN(CC2)CCOC3=CC=C(C=C3)O)O.Cl
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| InChi Key |
WFFZHKKSIDENAJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H27NO3.ClH/c1-17-2-4-18(5-3-17)16-21(24)10-12-22(13-11-21)14-15-25-20-8-6-19(23)7-9-20;/h2-9,23-24H,10-16H2,1H3;1H
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| Chemical Name |
1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]piperidin-4-ol;hydrochloride
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| Synonyms |
RO-63-1908 CO-101244 HCl CO-101244 hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~264.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6462 mL | 13.2310 mL | 26.4620 mL | |
| 5 mM | 0.5292 mL | 2.6462 mL | 5.2924 mL | |
| 10 mM | 0.2646 mL | 1.3231 mL | 2.6462 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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