187523-35-9

中文名稱 (3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one

英文名稱 (3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one

CAS 187523-35-9

分子式 C16H10ClF4NO2

分子量 359.7

MOL 文件 187523-35-9.mol

更新日期 2024/11/07 23:03:30

187523-35-9 結構式

基本信息物理化學性質安全數據圖譜信息常見問題列表

基本信息

中文別名

化合物FLINDOKALNER

英文別名

MaxiPost
FLINDOKALNER
BMS-204352 (BMS 204352
(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one
(3S)-3-(5-Chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-2H-Indol-2-one
2H-Indol-2-one, 3-(5-chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-, (3S)-

物理化學性質

沸點436.9±45.0 °C(Predicted)

密度1.50±0.1 g/cm3(Predicted)

儲存條件-20°C儲存

溶解度Soluble to 100 mM in DMSO and to 100 mM in ethanol

酸度系數(pKa)10.43±0.40(Predicted)

形態(tài)粉末

顏色White to off-white

安全數據

危險性符號(GHS) GHS hazard pictograms

GHS07

警示詞警告

危險性描述H315-H319-H335

防范說明P261-P264-P271-P280-P302+P352-P305+P351+P338

圖譜信息

(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one(187523-35-9)核磁圖(¹HNMR)

常見問題列表

生物活性

Flindokalner (BMS-204352) 是鉀離子通道 (potassium channel) 調節(jié)劑。Flindokalner 是在 HEK293 細胞中表達的所有神經元 Kv7 通道亞型的正調節(jié)劑。Flindokalner 是一種大電導鈣激活 K 通道 (BKca) 正向調節(jié)劑。Flindokalner 在 Kv7.1 通道 (Ki=3.7 μM) 處顯示負調節(jié)活性，并充當 GABAA 受體的負調節(jié)劑。Flindokalner 在體內顯示出抗焦慮功效。

靶點

Ki: 3.7 μM (Kv7.1), 230 μM (Kv7.4), 605 μM (Kv7.5)

體外研究

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.

體內研究

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.