中文名 | VERNAKALANT HYDROCHLORIDE |
英文名 | VERNAKALANT HYDROCHLORIDE |
别名 | 盐酸维那卡兰 盐酸弗纳卡兰 盐酸维纳卡兰 化合物 T17227 |
英文别名 | D06665 Vernakalant HCl RSD1235 hydrochloride RSD 1235 hydrochloride RSD-1235 hydrochloride VERNAKALANT HYDROCHLORIDE Vernakalant hydrochloride (usan) Vernakalant ((3R,1'R,2'R)-Isomer) HCl |
CAS | 748810-28-8 |
化学式 | C20H32ClNO4 |
分子量 | 385.93 |
熔点 | 151-153oC |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
存储条件 | Hygroscopic, Refrigerator, under inert atmosphere |
外观 | 固体 |
颜色 | White to Pale Yellow |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.591 ml | 12.956 ml | 25.911 ml |
5 mM | 0.518 ml | 2.591 ml | 5.182 ml |
10 mM | 0.259 ml | 1.296 ml | 2.591 ml |
5 mM | 0.052 ml | 0.259 ml | 0.518 ml |
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