Nelonemdaz
Based on 1 Customer Validation
Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death.
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- Pureza: 99.84%
- No. CAS: 640290-67-1
- Fòrmula: C15H8F7NO3
- Peso molecular:383.22
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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NMDA Receptor |
Nelonemdaz (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM[1].
Nelonemdazl (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner[1].
Nelonemdaz (0.1-1 μM) produces a marked reduction of Fe2+-induced neurotoxicity, even at doses of 0.1 to 0.3 μM[1].
Nelonemdaz (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures[1].
Nelonemdaz (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 (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 (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC50 of 2.72±0.26 μM[3].
Nelonemdaz (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 (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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No. CAS 640290-67-1
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Appearance Solid
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Peso molecular 383.22
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Fòrmula C15H8F7NO3
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Color Off-white to light yellow
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SMILES
OC(C1=C(O)C=CC(NCC2=C(C(F)=C(C(F)(F)F)C(F)=C2F)F)=C1)=O
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Synonyms
Salfaprodil free base; Neu2000
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : ≥ 112.5 mg/mL (293.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6095 mL | 13.0473 mL | 26.0947 mL | 65.2367 mL |
| 5 mM | 0.5219 mL | 2.6095 mL | 5.2189 mL | 13.0473 mL | |
| 10 mM | 0.2609 mL | 1.3047 mL | 2.6095 mL | 6.5237 mL | |
| 15 mM | 0.1740 mL | 0.8698 mL | 1.7396 mL | 4.3491 mL | |
| 20 mM | 0.1305 mL | 0.6524 mL | 1.3047 mL | 3.2618 mL | |
| 25 mM | 0.1044 mL | 0.5219 mL | 1.0438 mL | 2.6095 mL | |
| 30 mM | 0.0870 mL | 0.4349 mL | 0.8698 mL | 2.1746 mL | |
| 40 mM | 0.0652 mL | 0.3262 mL | 0.6524 mL | 1.6309 mL | |
| 50 mM | 0.0522 mL | 0.2609 mL | 0.5219 mL | 1.3047 mL | |
| 60 mM | 0.0435 mL | 0.2175 mL | 0.4349 mL | 1.0873 mL | |
| 80 mM | 0.0326 mL | 0.1631 mL | 0.3262 mL | 0.8155 mL | |
| 100 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6524 mL |
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