NBQX (FG9202)

製品コードS9686 バッチS968601

印刷

化学情報

 Chemical Structure Synonyms NNC 079202 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C12H8N4O6S

分子量 336.28 CAS No. 118876-58-7
Solubility (25°C)* 体外 DMSO 67 mg/mL (199.23 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

3.35mg/ml (9.96mM) Taking the 1 mL working solution as an example, add 50 μL of 67 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

3.35mg/ml (9.96mM) Taking the 1 mL working solution as an example, add 50 μL of 67 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
in vitro

NBQX (FG9202) is highly selective in vitro. The IC50 value for inhibition of AMPA-evoked inward currents is 0.4 μM for this compound. While it inhibits NMDA-induced currents with IC50 value of 60 μM.[2]

in vivo

Rats are intraperitoneally (i.p.) injected with pentylenetetrazole (PTZ, 50 mg/kg) for 28 consecutive days to establish chronic epilepsy models. Subsequently, NBQX (FG9202, 20 mg/kg, i.p.) is injected for 3 days for the observation of behavioral measurements of epilepsy. This compound treatment normalizes perineuronal nets (PNNs), tenascin-R, aggrecan and neurocan levels. It is sufficient to decrease seizures through increasing the latency to seizures, decrease the duration of seizure onset, and reduce the scores for the severity of seizures.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Mouse neocortical neurones
濃度 0.1 μM - 100 μM
反応時間 --
実験の流れ

Cells are continuously superfused with extracellular saline at a rate of 2.5 ml/min. After giga-seal formation the whole cell configuration is obtained by suction.The holding potential is - 60 mV and at the start of each experiment the current is measured continuously for 30 s to ensure a stable baseline. Agonist-containing solutions are delivered to the chamber through a custom-made gravity-driven flowpipe, the tip of which is placed approximately 50 μm from the cell. Application is triggered when the tubing connected to the flowpipe is compressed by a valve controlled by the Pulse software. In general, agonists are applied for 1.5 or 3 s every 45 s. The sample interval during application is 600 μs. After stable responses are obtained, the extracellular saline as well as the agonist-containing solution are replaced by solutions containing NBQX (FG9202). This compound is present until responses of a repeatable amplitude are achieved. Currents are measured at the plateau phase of the responses just before deactivation.

動物実験 動物モデル Male Wistar rats
投薬量 20 mg/kg
投与方法 IP

参考

  • https://pubmed.ncbi.nlm.nih.gov/27880801/
  • https://pubmed.ncbi.nlm.nih.gov/9726646/

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。