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  5. Ajmaline hydrochloride

Ajmaline hydrochloride  (Synonyms: Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride)

目录号: HY-B1167A
产品使用指南

Ajmaline hydrochloride 是一种Ia类抗心律失常试剂。它能抑制HERG钾通道,在HEK细胞和蛾蜘蛛卵母细胞中的IC50分别为1.0μmol/l和42.3μmol/l。Ajmaline hydrochloride 的抑制作用起效快、可逆,并呈正频率依赖性。它主要作用于HERG通道的开放状态,可能也结合于失活状态。Ajmaline hydrochloride 的抑制作用依赖S6结构域中的芳香族残基,并且在失活缺陷型HERG S620T通道中敏感性显著降低。它还可轻微影响HERG通道的激活电压。Ajmaline hydrochloride 对HERG通道的抑制作用可能既贡献于其高效的抗心律失常作用,也可能导致其潜在的促心律失常风险。

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Ajmaline hydrochloride Chemical Structure

Ajmaline hydrochloride Chemical Structure

CAS No. : 4410-48-4

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生物活性

Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.

分子量

362.89

Formula

C20H27ClN2O2

CAS 号
结构分类
初始来源
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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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

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Ajmaline hydrochloride
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