ICA-27243|cas:325457-89-4|西域试剂

ICA-27243,99.18%

产品编号：Bellancom-122114| CAS NO：325457-89-4| 分子式：C₁₂H₇ClF₂N₂O| 分子量：268.65

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货号	价格	库存与货期
Bellancom-122114	￥900.00	杭州北京（现货）
Bellancom-122114	￥1500.00	杭州北京（现货）
Bellancom-122114	￥5000.00	杭州北京（现货）
Bellancom-122114	￥8500.00	杭州北京（现货）

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ICA-27243

产品介绍

ICA-27243 是一种选择性，有效和口服活性的 KCNQ2/Q3 钾通道开放剂，EC₅₀ 为 0.38 μM。ICA-27243 在激活 KCNQ4 和 KCNQ3/Q5 方面效果较差。ICA-27243 具有抗癫痫和抗惊厥作用。

生物活性

ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC₅₀ of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects.

体外研究

In SH-SY5Y human neuroblastoma cells, ICA-27243 produces membrane potential hyperpolarization that could be prevented by coadministration with the M-current inhibitors XE-991 and Linopirdine. ICA-27243 enhances both ⁸⁶Rb⁺ efflux (EC₅₀ = 0.2 μM) and whole-cell currents in Chinese hamster ovary cells stably expressing heteromultimeric KCNQ2/Q3 channels (EC₅₀ = 0.4 μM). Activation of KCNQ2/Q3 channels is associated with a hyperpolarizing shift of the voltage dependence of channel activation (V_1/2 shift of -19 mV at 10 μM).

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

体内研究

ICA-27243 (1-100 mg/kg; oral administration; male CD-1 mice) has anticonvulsant activity (ED₅₀ of 8.4 mg/kg) in the mouse maximal electroshock epilepsy model.

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

Animal Model:	Male CD-1 mice with electroshock assay
Dosage:	1-100 mg/kg
Administration:	Oral administration
Result:	Produced a dose-dependent increase in the latency to hind limb extension, exhibiting an ED₅₀ value of 8.4 mg/kg.

体内研究

ICA-27243 (1-100 mg/kg; oral administration; male CD-1 mice) has anticonvulsant activity (ED₅₀ of 8.4 mg/kg) in the mouse maximal electroshock epilepsy model.

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

Animal Model:	Male CD-1 mice with electroshock assay
Dosage:	1-100 mg/kg
Administration:	Oral administration
Result:	Produced a dose-dependent increase in the latency to hind limb extension, exhibiting an ED₅₀ value of 8.4 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (930.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7223 mL	18.6116 mL	37.2232 mL
5 mM	0.7445 mL	3.7223 mL	7.4446 mL
10 mM	0.3722 mL	1.8612 mL	3.7223 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 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.74 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.74 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。