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。
产品描述
Vernakalant Hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker.
体外活性
Block of Kv1.5 by Vernakalant Hydrochloride is mediated after channel activation because Vernakalant causes a relatively rapid onset of a block of channel current upon depolarization but little evidence of resting or “tonic” block of the channel. 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. 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 channels, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively [1].
Cas No.
748810-28-8
分子式
C20H32ClNO4
分子量
385.93
别名
RSD1235 hydrochloride
储存和溶解度
DMSO:45mg/mL (116.6mM),Need ultrasonic
H2O:45mg/mL (116.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years