Flindokalner BMS-204352|cas:187523-35-9|西域试剂

Flindokalner BMS-204352,99.42%

产品编号：Bellancom-108584| CAS NO：187523-35-9| 分子式：C₁₆H₁₀ClF₄NO₂| 分子量：359.70

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货号	价格	库存与货期
Bellancom-108584	￥1600.00	杭州北京（现货）
Bellancom-108584	￥2300.00	杭州北京（现货）
Bellancom-108584	￥4800.00	杭州北京（现货）
Bellancom-108584	￥8500.00	杭州北京（现货）
Bellancom-108584	￥14500.00	杭州北京（现货）

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Flindokalner BMS-204352

产品介绍

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 (K_i=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。

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 (K_i=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.

体外研究

Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with K_is 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (278.01 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7801 mL	13.9005 mL	27.8009 mL
5 mM	0.5560 mL	2.7801 mL	5.5602 mL
10 mM	0.2780 mL	1.3900 mL	2.7801 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (6.95 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.95 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.95 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。