2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. NMDA receptor antagonist 4

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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NMDA receptor antagonist 4 Chemical Structure

NMDA receptor antagonist 4 Chemical Structure

CAS No. : 1607589-56-9

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Based on 1 publication(s) in Google Scholar

NMDA receptor antagonist 4 Related Antibodies

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Description

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[1].

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.

NMDA receptor antagonist 4 Related Antibodies

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.
Molecular Weight

231.31

Formula

C15H18FN
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3232 mL 21.6160 mL 43.2320 mL
5 mM 0.8646 mL 4.3232 mL 8.6464 mL
View the 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.

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Purity & Documentation
References

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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NMDA receptor antagonist 4 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NMDA receptor antagonist 41607589-56-9NMDA receptor antagonist4NMDA receptor antagonist-4iGluRIonotropic glutamate receptorsC. elegans5XFADMemantine analogsInhibitorinhibitorinhibit

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