NMDA receptor antagonist 4
Based on 1 Customer Validation
NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 μM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease.
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- Pureza: 99.64%
- No. CAS: 1607589-56-9
- Fòrmula: C15H18FN
- Peso molecular:231.31
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Descripciòn
IC50 & Target
IC50: 1.93 µM (NMDAR)[1]
In Vitro
NMDA receptor antagonist 4 (IIc) shows competitive interaction with endogenous blocker Mg2+, and shows dependence on membrane potential in the NMDAR channel[1].
NMDA receptor antagonist 4 shows high metabolic stability in human and mice liver microsomes, and shows hERG safety, without obvious cytotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neuro2A cells
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Concentration:1, 10, and 100 µM
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Incubation Time:24 h
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Result:Did not show cytotoxic at the highest concentration tested (100 µM).
In Vivo
NMDA receptor antagonist 4 (5 mg/kg/day; p.o.; 4 weeks) improves cell survival and synaptic function in AD through increasing the activity of cell-survival signaling pathways (Fyn-GluN2B-CREB signaling) and preventing internalization of synaptic NMDARs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C. elegans (N2 wild-type, CL2006, CL2122, CL2355)[1]
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Dosage:0, 0.1, 0.5, 1.5, and 10 µM
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Administration:
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Result:Reduced defective locomotion in CL2006 nematodes. Significantly reversed the chemotaxis behavior of CL2355 nematodes disrupted by Aβ expression.
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Animal Model:Six months old female 5XFAD mice[1]
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Dosage:5 mg/kg/day
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Administration:Oral administration, 4 weeks
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Result:Enhanced working memory function. Rescued the expression of GluN2A and postsynaptic density protein (PSD) 95. Increased Fyn phosphorylated levels and correspondingly elevated GluN2B phosphorylation at Tyr1472. Significantly increased p-CREB protein levels in the nucleus. Reverted calbindin D-28K protein levels.
Chemical Information
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No. CAS 1607589-56-9
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Appearance Solid
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Peso molecular 231.31
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Fòrmula C15H18FN
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Color White to light yellow
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SMILES
NC12CC3C4=CC=CC=C4C(CC(F)(C2)C3)C1
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (540.40 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. 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. 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)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 4.3232 mL | 21.6160 mL | 43.2320 mL | 108.0801 mL |
| 5 mM | 0.8646 mL | 4.3232 mL | 8.6464 mL | 21.6160 mL | |
| 10 mM | 0.4323 mL | 2.1616 mL | 4.3232 mL | 10.8080 mL | |
| 15 mM | 0.2882 mL | 1.4411 mL | 2.8821 mL | 7.2053 mL | |
| 20 mM | 0.2162 mL | 1.0808 mL | 2.1616 mL | 5.4040 mL | |
| 25 mM | 0.1729 mL | 0.8646 mL | 1.7293 mL | 4.3232 mL | |
| 30 mM | 0.1441 mL | 0.7205 mL | 1.4411 mL | 3.6027 mL | |
| 40 mM | 0.1081 mL | 0.5404 mL | 1.0808 mL | 2.7020 mL | |
| 50 mM | 0.0865 mL | 0.4323 mL | 0.8646 mL | 2.1616 mL | |
| 60 mM | 0.0721 mL | 0.3603 mL | 0.7205 mL | 1.8013 mL | |
| 80 mM | 0.0540 mL | 0.2702 mL | 0.5404 mL | 1.3510 mL | |
| 100 mM | 0.0432 mL | 0.2162 mL | 0.4323 mL | 1.0808 mL |
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