产品
编 号：F234689
分子式：C16H10ClF4NO2
分子量：359.7
分子式：C16H10ClF4NO2
分子量：359.7
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 187523-35-9
产品详情
生物活性：
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
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.
体外研究：
Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with Kis of 230 and 605 μM, respectively.Flindokalner (1-10 μM) causes inhibition of the Ca2+ current in a dose-dependent manner, with a Kd of 6 μM and a Hill coefficient of 1.33. Flindokalnerinhibits cardiac L-type Ca2+ channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes.
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
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.
体外研究：
Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with Kis of 230 and 605 μM, respectively.Flindokalner (1-10 μM) causes inhibition of the Ca2+ current in a dose-dependent manner, with a Kd of 6 μM and a Hill coefficient of 1.33. Flindokalnerinhibits cardiac L-type Ca2+ channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes.
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