ICA-27243

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Chemical Structure| 325457-89-4 同义名 : -
CAS号 : 325457-89-4
货号 : A458603
分子式 : C12H7ClF2N2O
纯度 : 95%
分子量 : 268.647
MDL号 : MFCD17166959
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(930.59 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 value of 0.38 μM. ICA-27243 is less effective in activating KCNQ4 and KCNQ3/Q5. ICA-27243 exhibits antiepileptic and anticonvulsant effects[1][2]. In SH-SY5Y human neuroblastoma cells, ICA-27243 produces membrane potential hyperpolarisation, which is prevented in combination with the M-current inhibitors XE-991 and Linopirdine. In CHO cells stably expressing heterotrimeric KCNQ2/Q3 channels, ICA-27243 enhanced 86Rb+ efflux (EC50=0.2 μM) and whole-cell currents (EC50=0.4 μM). Activation of KCNQ2/Q3 channels was associated with a voltage-dependent hyperpolarising shift in channel activation (V1/2 shifted to -19 mV at 10 μM)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.72mL

0.74mL

0.37mL

18.61mL

3.72mL

1.86mL

37.22mL

7.44mL

3.72mL
参考文献

[1]Wickenden AD, et al. N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): a novel, selective KCNQ2/Q3 potassium channel activator. Mol Pharmacol. 2008 Mar;73(3):977-86.

[2]Amato G, et al. N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy. ACS Med Chem Lett. 2011 Mar 31;2(6):481-4.