Vernakalant Hydrochloride

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Vernakalant Hydrochloride

CAS No. : 748810-28-8

MCE 国际站：Vernakalant Hydrochloride

产品活性：Vernakalant hydrochloride 是一种混合电压和频率依赖性的 Na⁺ 和 K⁺ 通道阻断剂。Vernakalant 抑制 Kv1.5 channel^wt，Kv1.5 channel^I508F，Kv1.5 channel^T479A，IC₅₀ 分别为 13.35±0.93 μM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: Block of Kv1.5 by Vernakalant Hydrochloride is mediated after channel activation, because Vernakalant causes a relatively rapid onset of block of channel current upon depolarization but little evidence of resting or “tonic” block of the channel. In the presence of 10 μM Vernakalant, rapid block is apparent after channel opening, and a steady-state current level is rapidly reached. The most important effect is the reduction in potency for Vernakalant centered at I502A, which had an IC₅₀ of 329±19 μM (n=4-10), compared with a control IC₅₀ of 13.4±0.9 μM (n=5-23), which is a 25-fold decrease in potency. V505A, I508A, T480A, and C500A showed lesser reductions in potency on Kv1.5, of between 3- and 4-fold. I508Y in our experiments increased the IC₅₀ for Vernakalant on Kv1.5 to 24.7 μM, again similar to the reported value for hERG.

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