(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one
| 中文名称 | (3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one |
|---|---|
| 中文同义词 | 化合物FLINDOKALNER;MAXIPOST,钾通道调节剂 |
| 英文名称 | (3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one |
| 英文同义词 | (3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one;FLINDOKALNER;MaxiPost;(3S)-3-(5-Chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-2H-Indol-2-one;BMS-204352 (BMS 204352;2H-Indol-2-one, 3-(5-chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-, (3S)-;Flindokalner BMS-204352;inhibit,KcsA,Flindokalner,neuronal,ventricular,effects,BMS204352,anxiolytic,subtype,Potassium Channel,Inhibitor,BMS 204352,myocytes,current |
| CAS号 | 187523-35-9 |
| 分子式 | C16H10ClF4NO2 |
| 分子量 | 359.7 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 187523-35-9.mol |
| 结构式 |  |
(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one 性质
| 沸点 | 436.9±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.50±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 在 DMSO 中溶解度为 100 mM，在乙醇中溶解度为 100 mM |
| 形态 | 粉末 |
| 酸度系数(pKa) | 10.43±0.40(Predicted) |
| 颜色 | 白色至米白色 |
Ki: 3.7 μM (Kv7.1), 230 μM (Kv7.4), 605 μM (Kv7.5)
Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with K
i
s of 230 and 605 μM, respectively.
Flindokalner (1-10 μM) causes inhibition of the Ca
2+
current in a dose-dependent manner, with a Kd of 6 μM and a Hill coefficient of 1.33. Flindokalnerinhibits cardiac L-type Ca
2+
channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes.
Flindokalner (BMS-204352) (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect.
In shock-based conditioned model of anxiety in male Wistar rats, Flindokalner (3-60 mg/kg; i.p.) engenderes an anxiolytic profile.
| Animal Model: | Female NMRI or male C57 mice (20-25 g) (Anxiolytic Models) |
| Dosage: | i.p. |
| Administration: | 3, 10, 30 mg/kg |
| Result: | Significantly and dose dependently increased time spent in the open areas, reduced latency to enter an open area, and increased the number of entries in to the open areas in Zero Maze. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-108584 | Flindokalner | 1 mg | 727元 | |
| 2024/08/19 | HY-108584 | (3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one Flindokalner | 187523-35-9 | 5mg | 1600元 |