187523-35-9

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

英文名称 (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 2024/12/23 10:32:36

187523-35-9 结构式

基本信息物理化学性质安全数据图谱信息常见问题列表

基本信息

中文别名

化合物FLINDOKALNER

英文别名

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)-

物理化学性质

沸点436.9±45.0 °C(Predicted)

密度1.50±0.1 g/cm3(Predicted)

储存条件-20°C储存

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

酸度系数(pKa)10.43±0.40(Predicted)

形态粉末

颜色White to off-white

安全数据

危险性符号(GHS) GHS hazard pictograms

GHS07

警示词警告

危险性描述H315-H319-H335

防范说明P261-P264-P271-P280-P302+P352-P305+P351+P338

图谱信息

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

常见问题列表

生物活性

Flindokalner (BMS-204352) 是钾离子通道 (potassium channel) 调节剂。Flindokalner 是在 HEK293 细胞中表达的所有神经元 Kv7 通道亚型的正调节剂。Flindokalner 是一种大电导钙激活 K 通道 (BKca) 正向调节剂。Flindokalner 在 Kv7.1 通道 (Ki=3.7 μM) 处显示负调节活性，并充当 GABAA 受体的负调节剂。Flindokalner 在体内显示出抗焦虑功效。

靶点

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

体外研究

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.

体内研究

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.