GI-530159  ≥98%

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包装规格:5g 25g 100g in glass bottle
产品简介:一种选择性的TREK1(K2P2.1)和TREK2(K2P10.1)通道的开放剂,对TREK1的EC50为0.76μM。GI-530159显示了TREK1/2对TRAAK,TASK3和其他钾离子通道的选择性。GI-530159降低大鼠背根神经节神经元兴奋性。
溶解性:溶于DMSO(250mg/ml超声)
储备液保存:-80°C, 6 months -20°C, 1 month
靶点:Target: TREK1/2
体外研究:TREK (TWIK-related K) two pore domain potassium (K2P) channels regulate the excitability of somatosensory nociceptive neurons and mediate pain perception. GI-530159 (1 µM or 10 µM) shows selectivity and activates TREK1 and TREK2 channels but shows no significant effects on TRAAK channels or K channels tested. GI-530159 (0.1-30 µM) activates recombinant human TREK1 channels with EC50s of 0.8 µM and 0.9 µM from Rb efflux and electrophysiological experiments, respectively. GI-530159 (1 µM) reduces rat dorsal root ganglion (DRG) neuron excitability, results in firing frequency reduction and a small hyperpolarisation of resting membrane potential (RMP).
保存条件:室温
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。