GI-530159
目录号: PL09957 纯度: ≥98.0%
CAS No. :69563-88-8
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中文名称
GI-530159
中文别名
2,2-双[4-(4-氨基苯氧基)苯基]六氟丙烷;2,2-双【4-(4-氨基苯氧基)苯基】六氟丙烷;2,2-双[4-(4-氨基苯氧基)苯]六氟丙烷;2,2-双[4-(4-氨基苯氧基苯)]六氟丙烷;2,2-Bis[4-(4-aminophenoxy)phenyl]hexafluoropropane 2,2-双[4-(4-氨基苯氧基)苯]六氟丙烷;2,2-双[4-(4-氨基苯氧基)苯基]-1,1,1,3,3,3-六氟丙烷;2,2-双[4-(4-氨基苯氧基)苯基]六;2,2-双[4-(4-氨基苯氧基)苯基]六氟丙烷(HFBAPP);2,2-双[4-(4-氨基苯氧基苯)]六氟;4,4'-(((全氟丙烷-2,2-二基)双(4,1-亚苯基))双(氧基))二苯胺;六氟二胺;4,4'-(六氟异丙基)双(对苯氧基)二苯胺;4,4'-(六氟异亚甲基)双[(4-氨基苯氧基)苯];六氟二胺(HFBAPP)
英文名称
GI-530159
英文别名
2,2-Bis【4-(4-aminophenoxy)phenyl】-hexafluoropropanane;2,2-Bis[4-(-aminophenoxy)phenyl]hexafluoropropane;BAPOFP;4,4-(Hexafluoroisopropylidene)bis(p-phenylenoxy)dianiline;Bisaminophenoxyphenylhexafluoropropane;2,2-Bis[4-(4-aminophenoxy)phenyl]hexafluoropropane;2,2-Bis[4-(4-aminophenoxy)phenyl]-hexafluoropropanane;4,4'-(Hexafluoroisopropylidene)bis(P-phenyleneoxy)dianiline;2,2-BIS[4-(4'-AMINOPHENOXY)PHENYL]HEXAFLUOROPROPANE;[1,1-bis(trifluoromethyl)-1,1-bis(4-(4-amino-phenoxy)-phenyl)]methane;1,1,1,3,3,3-hexafluoro-2,2-bis[4-(4-aminophenoxy)phenyl]propane;2,2'-BIS[4-(4-AMINOPHENOXY)PHENY]HEXAFLUOROPROPANE;2,2-bis[4-(4'-aminophenoxy)phenyl]-1,1,1,3,3,3-hexafluoropropane;2,2-bis[4-(4-aminophenoxy)-phenyl]hexafluoropropane;2,2-bis[4-(p-aminophenoxy)phenyl]hexafluoropropane;4,4′-(Hexafluoroisopropylidene)bis(p-phenyleneoxy)dianiline;4-BDAF;BIS-AF-A;HFBAPP;isbenzenamine;4,4'-(Hexafluoroisopropylidene)bis[(4-aminophenoxy)benzene];4,4'-Hexafluoroisopropylidenebis(p-phenyleneoxy)dianiline;4,4'-[4,4'-(Perfluoropropane-2,2-diyl)bis(4,1-phenyleneoxy)]dianiline;4,4'-(((Perfluoropropane-2,2-diyl)bis(4,1-phenylene))bis(oxy))dianiline;HHLMWQDRYZAENA-UHFFFAOYSA-N;2,2-Bis(4-(4-aminophenoxy)phenyl)hexafluoropropane;2,2-Bis(4-[4-aminophenoxy]phenyl)hexafluoropropane;Benzenamine, 4,4'-[[2,2,2-trifluoro-1-(trifluoromethyl)ethylidene]bis(4,1-phenyleneoxy)]bis-;AK202702;4',4'''-(Hexafluoroisopropylidene)-bis-(4-phenoxyaniline);Benzenamine, 4,4'-((2,2,2-trifluoro-1-(trifluoromethyl)ethylidene)bis;GI-530159
Cas No.
69563-88-8
分子式
C27H20F6N2O2
分子量
518.45
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GI-530159 是选择性的 TREK1 和 TREK2 钾通道的开放剂。GI-530159 对 TREK1/2 的选择性高于 TRAAK、TASK3 和其他钾通道,对 TREK1 的 EC50 为 0.76 μM。GI-530159 能够降低大鼠背根神经节神经元兴奋性,具有潜在的镇痛作用。
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 EC 50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect.
性状
Solid
IC50 & Target[1][2]
Target: TREK1/2
体外研究(In Vitro)
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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Loucif AJC, et al. GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P ) channel opener, reduces rat dorsal root ganglion neuron excitability. Br J Pharmacol. 2018;175(12):2272-2283.
溶解度数据
In Vitro: DMSO : 250 mg/mL (482.21 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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