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Adekalant(又名H 345/52)是一种新型抗心律失常化合物,具有低促心律失常活性。该化合物浓度依赖性地阻断HERG携带的电流,其半抑制浓度(IC50)为230 nM。Adekalant优先与开放状态的通道结合,并显示出异常快的动力学特性,通道关闭时被捕获。在方波脉冲和动作电位夹持协议期间观察到Adekalant的电压独立行为。研究提出,通过阻断I(Kr)来延迟人类心肌的复极是Adekalant发挥作用的主要机制。Adekalant高效阻断I(Kr),相对较低效地阻断I(Ca),且能延迟心室复极,而不会显著增加时间或空间的离散度,也不诱发早期后除极或TdP。
Adekalant(又名H 345/52)是一种新型抗心律失常化合物,具有低促心律失常活性。该化合物浓度依赖性地阻断HERG携带的电流,其半抑制浓度(IC50)为230 nM。Adekalant优先与开放状态的通道结合,并显示出异常快的动力学特性,通道关闭时被捕获。在方波脉冲和动作电位夹持协议期间观察到Adekalant的电压独立行为。研究提出,通过阻断I(Kr)来延迟人类心肌的复极是Adekalant发挥作用的主要机制。Adekalant高效阻断I(Kr),相对较低效地阻断I(Ca),且能延迟心室复极,而不会显著增加时间或空间的离散度,也不诱发早期后除极或TdP。
产品描述 | Adekalant (also known as H 345/52) is an innovative antiarrhythmic compound characterized by minimal proarrhythmic activity. It blocks HERG-mediated currents in a concentration-dependent manner, with a half-maximal inhibitory concentration (IC50) of 230 nM. Adekalant binds preferentially to open channels and exhibits rapid kinetic behavior, being trapped when channels close. Its voltage-independent properties have been observed during square pulse and action potential clamp protocols. Research suggests that delaying the repolarization of human cardiac muscle through I(Kr) blockage is the primary mechanism of Adekalant’s action. It effectively blocks I(Kr) while having relatively low efficacy in blocking I(Ca), delaying ventricular repolarization without significantly increasing temporal or spatial dispersion and without inducing early afterdepolarizations or torsades de pointes (TdP). |
别名 | H-34552, H34552, H-345/52, H345/52, H 34552, H 345/52 |
分子量 | 401.5 |
分子式 | C22H31N3O4 |
CAS No. | 227940-00-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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