CO-101244 hydrochloride (CO101244) is a novel and potent antagonist of NR2B-containing NMDA receptors. Overactivation of NMDA receptors (NMDARs) is a critical early step in glutamate-evoked excitotoxic injury of CNS neurons.
Physicochemical Properties
| Molecular Formula | C21H27NO3.HCL |
| Molecular Weight | 377.90492 |
| Exact Mass | 377.175 |
| Elemental Analysis | C, 66.74; H, 7.47; Cl, 9.38; N, 3.71; O, 12.70 |
| CAS # | 193356-17-1 |
| Related CAS # | 193359-26-1;193356-17-1 (HCl); |
| PubChem CID | 6918426 |
| Appearance | Light yellow to yellow solid powder |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 6 |
| Heavy Atom Count | 26 |
| Complexity | 379 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | WFFZHKKSIDENAJ-UHFFFAOYSA-N |
| 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 |
| Chemical Name | 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]piperidin-4-ol;hydrochloride |
| Synonyms | RO-63-1908 CO-101244 HCl CO-101244 hydrochloride |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| ln Vitro | Co 101244 enhances neuroprotective effects and significantly decreases the rise in Ca2+ produced by NMDA [1]. |
| 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]. |
| References |
[1]. Coupling diverse routes of calcium entry to mitochondrial dysfunction and glutamate excitotoxicity. Proc Natl Acad Sci U S A. 2009 Jun 16;106(24):9854-9. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~100 mg/mL (~264.62 mM) |
| 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. 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. 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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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 |