鹽酸維那卡蘭

生物活性靶點(diǎn)體外研究 用途與合成方法 MSDS 鹽酸維那卡蘭價(jià)格(試劑級(jí)) 上下游產(chǎn)品信息

中文名稱	鹽酸維那卡蘭
中文同義詞	鹽酸維那卡蘭;鹽酸弗納卡蘭;鹽酸維納卡蘭;化合物 T17227;(R)-1-((1R,2R)-2-(3,4-二甲氧基苯乙氧基)環(huán)己基)吡咯烷-3-醇鹽酸鹽
英文名稱	VERNAKALANT HYDROCHLORIDE
英文同義詞	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號(hào)	748810-28-8
分子式	C20H32ClNO4
分子量	385.93
EINECS號(hào)
相關(guān)類別
Mol文件	748810-28-8.mol
結(jié)構(gòu)式

鹽酸維那卡蘭 性質(zhì)

鹽酸維那卡蘭 用途與合成方法

生物活性

Vernakalant hydrochloride 是一種混合電壓和頻率依賴性的 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.

安全信息

MSDS信息

鹽酸維那卡蘭 價(jià)格(試劑級(jí))

鹽酸維那卡蘭 上下游產(chǎn)品信息