2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. GluN2B-NMDAR antagonist-2

GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke.

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GluN2B-NMDAR antagonist-2 Chemical Structure

GluN2B-NMDAR antagonist-2 Chemical Structure

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GluN2B-NMDAR antagonist-2 Related Antibodies

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Description

GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke[1].

IC50 & Target

GluN2B

74.01 nM (IC50)

In Vitro

GluN2B-NMDAR antagonist-2 (compound S-58) (1, 3, 10 µM) shows no significant prolonging effect on the action potential duration (APD90) in hiPSC-CMs[1].
GluN2B-NMDAR antagonist-2 (0-300 µM; 48 h) shows mild cytotoxicity for primary mouse neuron, VERO, L929, HEK293 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GluN2B-NMDAR antagonist-2 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: primary mouse neuron, VERO, L929, HEK293 cells
Concentration: 0, 0.3, 1, 3, 10, 100, 300 µM
Incubation Time: 48 h
Result: Showed mild cytotoxicity for primary mouse neuron, VERO, L929, HEK293 cells with IC50s of >300, 109.66, 56.34, 22.01 µM, respectively.
In Vivo

GluN2B-NMDAR antagonist-2 (5, 10, 20 mg/kg; i.v.) decreases the cerebral infarction rates and neurologic deficit scores in a dose dependent manner in MCAO rat model[1].
GluN2B-NMDAR antagonist-2 (450, 900 mg/kg; i.v.) shows a good safety profile with maximum tolerated dose (MTD) of 450 mg/kg in ICR mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Fifty-six Sprague-Dawley rats (MCAO rat model)[1]
Dosage: 5, 10, 20 mg/kg
Administration: I.v.
Result: Significantly decreased the cerebral infarction rates and neurologic deficit scores in a dose dependent manner, dramatically improved motor function, decreased cerebral infarct volume, and reduced neurologic scores, significantly reduced the Ca2+ concentration in brain tissue.
Molecular Weight

474.38

Formula

C24H25Cl2N3O3
SMILES

O=C(C1=CC=CC=C12)O[C@H]2CCCN(CC3)CCN3C(C4=CC(C=CC=C5Cl)=C5N4)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GluN2B-NMDAR antagonist-2 Related Classifications

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Help & FAQs
  • 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:

GluN2B-NMDAR antagonist-2iGluRIonotropic glutamate receptorsVEROL929HEK293 cellanti-strokeMCAO rat modelblood-brain barrierInhibitorinhibitorinhibit

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