Vernakalant Hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 channelwt，Kv1.5 channelI508F，Kv1.5 channelT479A，IC50 分别为 13.35±0.93 μM。

Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channelwt, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively.

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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Membrane Transporter/Ion Channel

Sodium Channel

Sodium Channel | Potassium Channel

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748810-28-8

385.93

C20H32ClNO4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (129.56 mM; 超声助溶 ) H2O 中的溶解度 : 50 mg/mL (129.56 mM; 超声助溶)

Cl.COc1ccc(CCO[C@@H]2CCCC[C@H]2N2CC[C@@H](O)C2)cc1OC

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(-20℃)

With Ice Pack

≥ 2 years