(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one
- CAS号:187523-35-9
- 英文名:(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one
- 中文名:(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one
- CBNumber:CB21253977
- 分子式:C16H10ClF4NO2
- 分子量:359.7
- MOL File:187523-35-9.mol
- 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 :Soluble to 100 mM in DMSO and to 100 mM in ethanol
- 形态 :Powder
- 酸度系数(pKa) :10.43±0.40(Predicted)
- 颜色 :White to off-white
(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one性质、用途与生产工艺
- 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。
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靶点
Ki: 3.7 μM (Kv7.1), 230 μM (Kv7.4), 605 μM (Kv7.5)
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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.
- 更新日期:2024/11/08
- 产品编号:HY-108584
- 产品名称:Flindokalner
- CAS编号:
- 包装:1 mg
- 价格:727元
- 更新日期:2024/11/08
- 产品编号:HY-108584
- 产品名称:(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one Flindokalner
- CAS编号:187523-35-9
- 包装:5mg
- 价格:1600元
- 公司名称:Axon Medchem BV
- 联系电话:--
- 电子邮件:info@axonmedchem.com
- 国家:荷兰
- 产品数:477
- 优势度:30