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Art. -Nr.: HY-146588

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NMDA receptor antagonist 4

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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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Reinheit: 99.64%
CAS. Nr.: 1607589-56-9
Formel: C₁₅H₁₈FN
Molecular Weight:231.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NMDA receptor antagonist 4 Chemical Structure

CAS. Nr.: 1607589-56-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 1.93 µM (NMDAR)^[1]

Alle iGluR Isoform-spezifische Produkte anzeigen :

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.

Cell Cytotoxicity Assay^[1]

Cell Line:

Neuro2A cells
Concentration:

1, 10, and 100 µM
Incubation Time:

24 h
Result:

Did not show cytotoxic at the highest concentration tested (100 µM).

In Vivo

NMDA receptor antagonist 4 (IIc) (0-10 μM) rescues the motor deficits, and protects against Aβ toxicity-related neuronal dysfunction^[1].
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.

Animal Model:

C. elegans (N2 wild-type, CL2006, CL2122, CL2355)^[1]
Dosage:

0, 0.1, 0.5, 1.5, and 10 µM
Administration:
Result:

Reduced defective locomotion in CL2006 nematodes. Significantly reversed the chemotaxis behavior of CL2355 nematodes disrupted by Aβ expression.

Animal Model:

Six months old female 5XFAD mice^[1]
Dosage:

5 mg/kg/day
Administration:

Oral administration, 4 weeks
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

CAS. Nr. 1607589-56-9
Appearance Solid
Molecular Weight 231.31
Formel C₁₅H₁₈FN
Color White to light yellow
SMILES

NC12CC3C4=CC=CC=C4C(CC(F)(C2)C3)C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.3232 mL

21.6160 mL

43.2320 mL

5 mM

0.8646 mL

4.3232 mL

8.6464 mL

10 mM

0.4323 mL

2.1616 mL

4.3232 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Andreea L. Turcu, et al. Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease. Eur J Med Chem. 2022 Apr 8;236:114354. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
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NMDA receptor antagonist 4

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NMDA receptor antagonist 4

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NMDA receptor antagonist 4 Related Classifications

HY-146588 Related Classifications