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Flindokalner (BMS-204352) 是一种钾离子通道调节剂。它是大电导钙激活 K 通道正向调节剂。它是在 HEK293 细胞中表达的所有神经元 Kv7通道亚型的正调节剂。它在 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。它在体内显示出抗焦虑功效。
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Flindokalner (BMS-204352) 是一种钾离子通道调节剂。它是大电导钙激活 K 通道正向调节剂。它是在 HEK293 细胞中表达的所有神经元 Kv7通道亚型的正调节剂。它在 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。它在体内显示出抗焦虑功效。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 337 | 现货 | |
5 mg | ¥ 768 | 现货 | |
10 mg | ¥ 1,090 | 现货 | |
25 mg | ¥ 2,350 | 现货 | |
50 mg | ¥ 3,370 | 现货 | |
100 mg | ¥ 4,720 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner displays a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM) and acts as a negative modulator of GABAA receptors and it also shows anxiolytic efficacy in vivo. |
靶点活性 | Kv7.1:3.7 μM(Ki), Kv7.4:230 μM(Ki), Kv7.5:605 μM(Ki) |
体外活性 | Flindokalner inhibits cardiac L-type Ca2+ channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes. Flindokalner (10 μM) inhibits Kv7.4and Kv7.5 (Kis: 230 and 605 μM, respectively)[1]. Flindokalner (1-10 μM) causes inhibition of the Ca2+ current in a dose-dependent manner (Kd: 6 μM and a Hill coefficient: 1.33) [2]. |
体内活性 | Flindokalner (3-60 mg/kg; i.p.) engenders an anxiolytic profile, in a shock-based conditioned model of anxiety in male Wistar rats. Flindokalner (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect [1]. |
别名 | BMS-204352 |
分子量 | 359.7 |
分子式 | C16H10ClF4NO2 |
CAS No. | 187523-35-9 |
Smiles | COc1ccc(Cl)cc1[C@]1(F)C(=O)Nc2cc(ccc12)C(F)(F)F |
密度 | 1.50 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (278.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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