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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 245063-59-6
- 分子式: C24H28N4O7S
- 分子量:516.57
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 245063-59-6
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分子量 516.57
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分子式 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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別名
NS-1209
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)