SPD-502
SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity.
For research use only. We do not sell to patients.
- CAS No.: 245063-59-6
- Formula: C24H28N4O7S
- Molecular Weight:516.57
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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
Description
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 245063-59-6
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Molecular Weight 516.57
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Formula C24H28N4O7S
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SMILES
O=C(N1)/C(C2=C1C3=C(C(C4=CC=C(S(N(C)C)(=O)=O)C=C4)=C2)CCN(C)C3)=N\OC(C(O)=O)CCO
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Synonyms
NS-1209
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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.
Protocols
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Primary Embryonic Cortical Neuron Culture
Primary embryonic cortical neuron culture isolates cortical tissue from prenatal rodents, dissociates it into single cells, and maintains neurons in vitro so that neurite extension, neuronal marker expression, synapse formation, survival, and treatment responses can be examined outside the intact brain.
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Primary Embryonic Hippocampal Neuron Culture
Primary embryonic hippocampal neuron culture is an in vitro method in which hippocampi from embryonic rodents are dissected, enzymatically or mechanically dissociated, plated on adhesive substrates, and maintained in defined neuronal medium or in low-density sandwich/co-culture formats to support neuronal attachment, neurite extension, polarity formation, dendritic arborization, and synapse formation. The main readouts are cell survival, neuronal purity, neurite outgrowth, axon-dendrite polarization, synaptic marker development, and functional neuronal activity, assessed by phase-contrast microscopy, immunocytochemistry for neuronal/glial markers, live imaging, or electrophysiology depending on the downstream experiment.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)