产品
编 号：F429237
分子式：C27H20F6N2O2
分子量：518.45
分子式：C27H20F6N2O2
分子量：518.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1g
200
In-stock
5g
400
In-stock
结构图
CAS No: 69563-88-8
产品详情
生物活性：
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect.
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).
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect.
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).
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