2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. azo-Q2a

azo-Q2a 是一种可光切换的 NaV1.5 抑制剂。azo-Q2a 在黑暗环境或 480 nm 光照下以反式异构体形式存在，活性较低；在 365 nm 光照下以顺式异构体形式存在，抑制效力更高。azo-Q2a 以光依赖的方式降低活体斑马鱼幼鱼的心率。azo-Q2a 可用于心律失常的研究。

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azo-Q2a

azo-Q2a Chemical Structure

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azo-Q2a 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

azo-Q2a is a photoswitchable NaV1.5 inhibitor. azo-Q2a exists as the trans isomer with low activity in the dark or under 480 nm illumination, and exists as the cis isomer with higher inhibitory potency under 365 nm illumination. azo-Q2a reduces the heart rate of living zebrafish larvae in a light-dependent manner. azo-Q2a can be used for the study of arrhythmias[1].

体外研究
(In Vitro)

Azo-Q2a (膜片钳记录期间给药 10 μM) 可对 HEK293T 细胞中的 NaV1.5 通道实现可逆的、光依赖型抑制；经 365 nm 光照形成的顺式 azo-Q2a 的效力比黑暗/480 nm 光照条件下产生的反式 azo-Q2a 高 7 倍，前者的 IC50 为 11.76 μM，后者的 IC50 为 81.58 μM，且该过程不会改变通道的激活特性[1]。
Azo-Q2a (膜片钳记录期间使用 10 μM) 在 HEK293T 和 CHO 细胞中对 NaV1.5 表现出高于其他 NaV 亚型及心脏离子通道的高光依赖选择性[1]。

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

azo-Q2a 相关抗体:
体内研究
(In Vivo)

Azo-Q2a (10 μM; soaked; dark incubation for 1-1.5 h) 可实现对斑马鱼幼鱼心率的可逆光调控：在 365 nm 光照下其心率可降至基础水平的 56.5%，在 480 nm 光照下则恢复至基础水平[1]。
Azo-Q2a (10 μM; 心动过速诱导后施加；365 nm 光照 5 min (cis isomer)；暗孵育 (trans isomer)) 在经 365 nm 光照激活为顺式异构体时，可有效终止异异丙肾上腺素诱导的斑马鱼幼鱼心动过速，将心率降至基线水平的 35.3%，而黑暗环境中的反式异构体仅产生极微弱的作用[1]。

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

Animal Model: AB strain (2 days post-fertilization larvae, gender not screened)[1]
Dosage: 10 μM
Administration: soaked; dark incubation for 1-1.5 h
Result: Had no significant effect on heart rate, with values measured at 98.8% of control baseline.
Reduced heart rate significantly to 56.5% of baseline after 365 nm illumination.
Restored heart rate to 103.2% of baseline after subsequent 480 nm illumination.
Animal Model: AB strain (3-4 days post-fertilization larvae, gender not screened)[1]
Dosage: 10 μM
Administration: applied after tachycardia induction; 365 nm illumination for 5 min (cis isomer); dark incubation (trans isomer)
Result: Markedly attenuated tachycardic heart rate to 35.3% of baseline under 365 nm illumination (cis isomer).
Produced only a mild 4.4% reduction in tachycardic heart rate in the dark (trans isomer).
分子量

504.62

Formula

C32H32N4O2
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

azo-Q2a 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

azo-Q2aSodium ChannelNa channelsNa+ channelszebrafish larvaecardiac ion channelsCHO cellsarrhythmiasHEK293T cellsNaV1 subtypesInhibitorinhibitorinhibit

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