1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. QO-83

QO-83 ,一种 Retigabine 类似物,是一种电压门控钾离子通道 KCNQ2 (Kv7.2) 激活剂,其 EC50 为 0.56 μM。QO-83 与处于闭合构象的 KCNQ2-CaM 复合物的单个疏水口袋结合。QO-83 可使 KCNQ2 通道的电压依赖性激活曲线向负方向偏移,提高通道的电压敏感性。QO-83 可用于癫痫的研究。

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QO-83

QO-83 Chemical Structure

CAS No. : 2253948-15-9

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  • 生物活性

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  • 参考文献

生物活性

QO-83, Retigabine analogue, is a voltage-gated potassium channel KCNQ2 (Kv7.2) activator with an EC50 of 0.56 μM. QO-83 binds to a single hydrophobic pocket of KCNQ2-CaM complex in closed conformation. QO-83 induces a negative shift in the voltage-dependent activation curve of KCNQ2 channels, increasing the channel's voltage sensitivity. QO-83 can be used for the research of epilepsies[1].

IC50 & Target[1]

KV7.2

0.56 μM (EC50)

体外研究
(In Vitro)

QO-83 (20 μM; 1 h) 结合于处于闭合构象的人源 KCNQ2-CaM 复合体 PD 结构域 (S5-S6 界面) 的单个疏水口袋,可引发 PD 结构域与 VSD 结构域 (S3-S4 界面) 的构象重排[1]
QO-83 (10 μM) 使电压依赖性激活曲线向负方向偏移[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

423.45

Formula

C22H25F4N3O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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HY-181128
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