Nelonemdaz potassium
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Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death.
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- Pureté: 99.86%
- CAS No.: 916214-57-8
- Formule: C15H7F7KNO3
- Masse moléculaire:421.31
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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NMDA Receptor |
Nelonemdaz potassium (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM[1].
Nelonemdaz potassium (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner[1].
Nelonemdaz potassium (0.1-1 μM) produces a marked reduction of Fe2+-induced neurotoxicity, even at doses of 0.1 to 0.3 μM[1].
Nelonemdaz potassium (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures[1].
Nelonemdaz potassium (0-350 μM) effectively scavenges superoxide radicals (IC50=63.07±1.44 μM), nitric oxide (IC50=155.8±4.88 μM), and hydroxyl radicals (IC50=58.45±1.74 μM)[3].
Nelonemdaz potassium (0.78-12.5 μM) decreases the amount of antimycin A-induced ROS/RNS formation in a dose-dependent manner, with an IC50 of 2.21±0.11 μM[3].
Nelonemdaz potassium (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC50 of 2.72±0.26 μM[3].
Nelonemdaz potassium (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC50=24.56±0.07 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nelonemdaz potassium (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (260 to 300 g) (clip occlusion model)[1]
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Dosage:0.5-20 mg/kg
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Administration:I.v. administration 5 mins after reperfusion
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Result:Produced a large neuroprotective effect, with a maximal reduction in infarct volume of 66% at doses of 2.5 to 5 mg/kg.
Not observed neuronal damage in the most vulnerable cortical area after administration of 5 mg/kg.
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Animal Model:Male Sprague-Dawley rats (260 to 300 g) (intraluminal thread occlusion model)[1]
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Dosage:5 mg/kg
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Administration:I.v. administration 30 mins after reperfusion
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Result:Did not change physiologic variables such as arterial pH, PCO2, PO2, and hematocrit.
Reduced infarct volume evolving in the cortex and the striatum substantially.
Reduced white matter damage in the striatum and external capsule markedly.
Chemical Information
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CAS No. 916214-57-8
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Appearance Solid
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Masse moléculaire 421.31
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Formule C15H7F7KNO3
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Color Off-white to light yellow
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SMILES
OC1=CC=C(C=C1C(O[K])=O)NCC2=C(C(F)=C(C(F)=C2F)C(F)(F)F)F
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Synonyms
Salfaprodil; Neu2000 potassium
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 200 mg/mL (474.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gwag BJ, et al. Marked prevention of ischemic brain injury by Neu2000, an NMDA antagonist and antioxidant derived from aspirin and sulfasalazine. J Cereb Blood Flow Metab. 2007 Jun;27(6):1142-51. [Content Brief]
[2]. Sung IC, et, al. Neu2000, an NR2B-selective, Moderate NMDA Receptor Antagonist and Potent Spin Trapping Molecule for Stroke. Drug News Perspect. 2010 Nov; 23(9): 549-56. [Content Brief]
[3]. Nishant PV, et, al. Antioxidant Properties of Neu2000 on Mitochondrial Free Radicals and Oxidative Damage. Toxicol In Vitro. 2013 Mar; 27(2): 788-97. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3735 mL | 11.8677 mL | 23.7355 mL | 59.3387 mL |
| 5 mM | 0.4747 mL | 2.3735 mL | 4.7471 mL | 11.8677 mL | |
| 10 mM | 0.2374 mL | 1.1868 mL | 2.3735 mL | 5.9339 mL | |
| 15 mM | 0.1582 mL | 0.7912 mL | 1.5824 mL | 3.9559 mL | |
| 20 mM | 0.1187 mL | 0.5934 mL | 1.1868 mL | 2.9669 mL | |
| 25 mM | 0.0949 mL | 0.4747 mL | 0.9494 mL | 2.3735 mL | |
| 30 mM | 0.0791 mL | 0.3956 mL | 0.7912 mL | 1.9780 mL | |
| 40 mM | 0.0593 mL | 0.2967 mL | 0.5934 mL | 1.4835 mL | |
| 50 mM | 0.0475 mL | 0.2374 mL | 0.4747 mL | 1.1868 mL | |
| 60 mM | 0.0396 mL | 0.1978 mL | 0.3956 mL | 0.9890 mL | |
| 80 mM | 0.0297 mL | 0.1483 mL | 0.2967 mL | 0.7417 mL | |
| 100 mM | 0.0237 mL | 0.1187 mL | 0.2374 mL | 0.5934 mL |
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