GYKI 52466
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research.
For research use only. We do not sell to patients.
- CAS No.: 102771-26-6
- Formula: C17H15N3O2
- Molecular Weight:293.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All iGluR Isoforms
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Biological Activity
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Kainate Receptor 11 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Neuron | IC50 |
10.8 μM
Compound: GYKI-52466
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Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay
Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay
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[PMID: 18083036] |
GYKI 52466 (0.3-100 μM) inhibits inward currents activated by AMPA and Kainate receptor in cultured rat hippocampal neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female DBA/2 mice tested for sound-induced seizure responses[2]
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Dosage:1.76-13.2 mg/kg
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Administration:Intraperitoneal injection; 1.76-13.2 mg/kg; once
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Result:Observed Maximal anticonvulsant protection after the i.p. treatment (5-15 min ).
Chemical Information
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CAS No. 102771-26-6
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Molecular Weight 293.32
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Formula C17H15N3O2
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SMILES
NC1=CC=C(C2=NN=C(C)CC3=CC4=C(OCO4)C=C32)C=C1
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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
[1]. S D Donevan, et al. GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses. Neuron. 1993 Jan;10(1):51-9. [Content Brief]
[2]. A G Chapman, et al. The anticonvulsant effect of the non-NMDA antagonists, NBQX and GYKI 52466, in mice. Epilepsy Res. 1991 Jul;9(2):92-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)