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.
For research use only. We do not sell to patients.
- CAS No.: 3034593-10-4
- Formula: C24H25Cl2N3O3
- Molecular Weight:474.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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GluN2B 74.01 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
22.01 μM
Compound: S-58
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Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
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[PMID: 38413367] |
| L929 | IC50 |
56.34 μM
Compound: S-58
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Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
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[PMID: 38413367] |
| Neuron | IC50 |
>300 μM
Compound: S-58
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Cytotoxicity against mouse primary neuron cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against mouse primary neuron cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
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[PMID: 38413367] |
| Vero | IC50 |
109.66 μM
Compound: S-58
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
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[PMID: 38413367] |
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.
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Cell Line:primary mouse neuron, VERO, L929, HEK293 cells
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Concentration:0, 0.3, 1, 3, 10, 100, 300 µM
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Incubation Time:48 h
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Result:Showed mild cytotoxicity for primary mouse neuron, VERO, L929, HEK293 cells with IC50s of >300, 109.66, 56.34, 22.01 µM, respectively.
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.
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Animal Model:Fifty-six Sprague-Dawley rats (MCAO rat model)[1]
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Dosage:5, 10, 20 mg/kg
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Administration:I.v.
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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.
Chemical Information
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CAS No. 3034593-10-4
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Molecular Weight 474.38
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Formula C24H25Cl2N3O3
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SMILES
O=C(C1=CC=CC=C12)O[C@H]2CCCN(CC3)CCN3C(C4=CC(C=CC=C5Cl)=C5N4)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GluN2B-NMDAR antagonist-2 Related Classifications
HY-157936 Related Classifications
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