CAS:489402-47-3ML 213

ML213 is an activator of Kv7.2 (KCNQ2) and Kv7.4 (KCNQ4) channels with EC50s of 230 and 510 nM respectively.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

489402-47-3

储存条件

分子式

C17H23NO

运输

蓝冰

分子量

257.37

别名

溶解度

DMSO	56.0 mg/mL (217.6 mM) warming
Water	insoluble

动物实验配方

生物活性

描述ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively. ML213 causes a concentration-dependent shift in the V1/2 for KCNQ2 activation with an EC50 of 340 ± 70 nM and a maximal shift of 37.4 mV^[3]. ML213 (100 nM-30 µM) increases maximal conductance to a peak at 212% ± 27% of control, with an EC50 of 0.8 ± 0.3 µM. ML213 (10 µM) reduces the deactivation rates of Kv7.4 currents by 4.6-fold in the voltage range from -130 mV to - 90 mV. ML213 is a potent and effective activator of homomeric Kv7.5 channels overexpressed in A7r5 cells. ML213 increases maximal conductance of Kv7.5 channels with an EC50 of 0.7 ± 0.2 µM. ML213 (10 µM) also reduces deactivation rates of Kv7.5 currents by 5.9-fold on average. ML213 produces similar effects on heteromeric Kv7.4/7.5 channels: 204% ± 11% maximal increase in conductance with an EC50 of 1.1 ± 0.6 µM and a 34.2 ± 3.3 mV maximal negative shift of the activation curve, with an EC50 of 3.8 ± 1.2 µM^[4]. ML213 causes a vasorelaxation in different precontracted rat blood vessels. ML213 (10 μM) also hyperpolarizes mesenteric artery smooth muscle cells^[5].