1. Membrane Transporter/Ion Channel
  2. Chloride Channel
  3. 19:0 Lyso PI-d5

AK-42 是一种选择性 CLC-2 氯离子通道抑制剂,对人源的 IC50 为 17 nM,对大鼠源的 IC50 为 14 nM。AK-42 结合于通道孔上方的细胞外前庭,可急性且可逆地抑制 CLC-2 电流,包括在辅助亚基 GlialCAM 共表达的情况下。AK-42 是用于急性调控 CLC-2 功能、探究 CLC-2 神经生理学特性的选择性工具化合物。AK-42 可用于脑白质营养不良和特发性全面性癫痫的相关研究。

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19:0 Lyso PI-d<sub>5</sub>

19:0 Lyso PI-d5 Chemical Structure

CAS No. : 15437-29-3

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  • 生物活性

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生物活性

AK-42 is a selective CLC-2 chloride channel inhibitor with human IC50 of 17 nM and rat IC50 of 14 nM. AK-42 binds to an extracellular vestibule above the channel pore, inhibits CLC-2 currents acutely and reversibly, including with auxiliary subunit GlialCAM coexpression. AK-42 acts as a selective tool compound for acute CLC-2 function modulation to probe CLC-2 neurophysiology. AK-42 can be used for the research of leukodystrophy and idiopathic generalized epilepsies[1].

IC50 & Target[1]

CLC-2

14 (rat) nM ()

CLC-2

17 (human) nM ()

体外研究
(In Vitro)

AK-42 (5 min) 可强效抑制稳定表达于 CHO 细胞中的人源 CLC-2 氯离子电流,其 IC50 为 17 nM;且对 CLC-1 的选择性超过 1000 倍,对其他中枢神经系统膜蛋白及阴离子通道的脱靶活性极低[1]
AK-42 可强效且可逆地抑制瞬时表达于 CHO 细胞中的大鼠 CLC-2 氯电流,其 IC50 为 14 nM,对与 GlialCAM 共表达的 CLC-2 具有相当的抑制效力,且其结合依赖于包括 K210 和 Q399 在内的特定细胞外通道残基[1]

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

分子量

388.24

Formula

C20H15Cl2NO3

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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19:0 Lyso PI-d5
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HY-182571
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