盐酸维那卡兰
生物活性靶点体外研究 用途与合成方法 MSDS 盐酸维那卡兰价格(试剂级) 上下游产品信息
中文名称 | 盐酸维那卡兰 |
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中文同义词 | 盐酸维那卡兰;盐酸弗纳卡兰;盐酸维纳卡兰;化合物 T17227;(R)-1-((1R,2R)-2-(3,4-二甲氧基苯乙氧基)环己基)吡咯烷-3-醇盐酸盐 |
英文名称 | VERNAKALANT HYDROCHLORIDE |
英文同义词 | RSD 1235 hydrochloride;RSD1235 hydrochloride;RSD-1235 hydrochloride;Vernakalant ((3R,1'R,2'R)-Isomer) HCl;Vernakalant HCl;VERNAKALANT HYDROCHLORIDE;D06665;Vernakalant hydrochloride (usan) |
CAS号 | 748810-28-8 |
分子式 | C20H32ClNO4 |
分子量 | 385.93 |
EINECS号 | |
相关类别 | |
Mol文件 | 748810-28-8.mol |
结构式 | ![]() |
盐酸维那卡兰 性质
熔点 | 151-153oC |
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储存条件 | Hygroscopic, Refrigerator, under inert atmosphere |
溶解度 | 可溶于DMSO(少许)、甲醇(少许) |
形态 | 固体 |
颜色 | 白色至浅黄色 |
盐酸维那卡兰 用途与合成方法
生物活性
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 channelwt,Kv1.5 channelI508F,Kv1.5 channelT479A,IC50 分别为 13.35±0.93 μM。
靶点
IC50: 13.35±0.93 μM (Kv1.5 channel wt ), 0.61±0.03 μM ( I508F ), 1.63±0.09 μM (Kv1.5 channel T479A )
体外研究
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 IC 50 of 329±19 μM (n=4-10), compared with a control IC 50 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 IC 50 for Vernakalant on Kv1.5 to 24.7 μM, again similar to the reported value for hERG.
安全信息
MSDS信息
盐酸维那卡兰 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-14183 | 盐酸维那卡兰 Vernakalant Hydrochloride | 748810-28-8 | 2mg | 950元 |
2024/08/19 | HY-14183 | 盐酸维那卡兰 Vernakalant Hydrochloride | 748810-28-8 | 5mg | 1800元 |