|N-(2-氯-5-嘧啶基)-3,4-二氟苯甲酰胺|CsnPharm

CAS No.: 582323-16-8

ICA-069673 Catalog No. CSN20444

ICA 069673 selectively inhibit KV7.2 (KCNQ2) and KV7.3 (KCNQ3) channel with EC50 of 0.69 μM and has no measurable activity over a panel of cardiac ion channels.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Potassium Channel KV7.2/7.3

EC50:0.69μM
描述ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM. In contrast, ICA-27243 was less effective at activating KCNQ4 and KCNQ3/Q5 and was selective over a wide range of neurotransmitter receptors and ion channels such as voltage-dependent sodium channels and GABA-gated chloride channels. ICA-27243 (1-10 mM) was found to reversibly suppress seizure-like activity in an ex vivo hippocampal slice model of epilepsy and demonstrated in vivo anticonvulsant activity (ED50 = 8.4 mg/kg) in the mouse maximal electroshock epilepsy model^[3]. In contrast to ML213, ICA-069673 robustly activated Kv7.4 channels but was significantly less effective on homomeric Kv7.5 channels. Heteromeric Kv7.4/7.5 channels displayed intermediate responses to ICA-069673. In each case, ICA-069673 induced a negative shift of the activation curves without significantly increasing maximal conductance^[4]. ICA-069673 inhibited spontaneous phasic, pharmacologically induced, and nerve-evoked contractions in DSM (detrusor smooth muscle) isolated strips in a concentration-dependent manner. Under conditions of elevated extracellular K(+) (60 mM), the effects of ICA-069673 on DSM tonic contractions were significantly attenuated. ICA-069673 decreased the global intracellular Ca(2+) concentration in DSM cells, an effect blocked by the L-type Ca(2+) channel inhibitor nifedipine^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7087 mL
- 18.5436 mL
- 37.0872 mL
- 5 mM
- 0.7417 mL
- 3.7087 mL
- 7.4174 mL
- 10 mM
- 0.3709 mL
- 1.8544 mL
- 3.7087 mL

技术信息

CAS号

582323-16-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H6ClF2N3O

运输

蓝冰

分子量

269.63

别名

溶解度

DMSO	54.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	54.0 mg/mL (200.3 mM)

动物实验配方

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ICA-069673 Catalog No. CSN20444

靶点选择性

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