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748810-28-8

中文名稱(chēng) 鹽酸維那卡蘭
CAS 748810-28-8
分子式 C20H32ClNO4
分子量 385.93
MOL 文件 748810-28-8.mol
更新日期 2024/12/13 09:49:01
748810-28-8 結(jié)構(gòu)式 748810-28-8 結(jié)構(gòu)式

基本信息

中文別名
鹽酸弗納卡蘭
鹽酸維那卡蘭
英文別名
D06665
Vernakalant HCl
RSD1235 hydrochloride
RSD 1235 hydrochloride
RSD-1235 hydrochloride
VERNAKALANT HYDROCHLORIDE
Vernakalant hydrochloride (usan)
Vernakalant ((3R,1'R,2'R)-Isomer) HCl
RSD1235 HYDROCHLORIDE
RSD 1235 HYDROCHLORIDE
RSD-1235 HYDROCHLORIDE
(R)-1-((1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexyl)pyrrolidin-3-ol hydrochloride
鹽酸維那卡蘭價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-14183鹽酸維那卡蘭
Vernakalant Hydrochloride
748810-28-82mg950元
2024/11/08HY-14183鹽酸維那卡蘭
Vernakalant Hydrochloride
748810-28-85mg1800元
2024/11/08HY-14183鹽酸維那卡蘭
Vernakalant Hydrochloride
748810-28-810mM * 1mLin DMSO1980元

常見(jiàn)問(wèn)題列表

生物活性
Vernakalant hydrochloride 是一種混合電壓和頻率依賴(lài)性的 Na+ 和 K+ 通道阻斷劑。Vernakalant 抑制 Kv1.5 channelwt,Kv1.5 channelI508F,Kv1.5 channelT479A,IC50 分別為 13.35±0.93 μM。
靶點(diǎn)

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 )

體外研究

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.

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