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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-GI-530159
GI-530159

Chemical Structure : GI-530159

CAS No.: 69563-88-8

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GI-530159 (GI530159, ICA-069771)

货号: PC-62092Not For Human Use, Lab Use Only.

GI-530159 (ICA-069771) is a novel potent, selective, mechano-sensitive K2P channel (TERK) opener with EC50 of 1 uM for TERK1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GI-530159 (ICA-069771) is a novel potent, selective, mechano-sensitive K2P channel (TERK) opener with EC50 of 1 uM for TERK1.
GI-530159 shows no activator effects on other potassium channels TASK2, KCNQ1, KCNQ2, KCNQ3 using Rb+ efflux assays or against NaV1.2, NaV1.7 and NaV1.8 (EC50>100 uM).
GI-530159 enhances TREK2 channels at 1 uM about 42 ± 6 %, but without effect on TRAAK and TASK3 channels.
GI-530159 shows a significant reduction in firing frequency and a small hyperpolarization of resting membrane potential in cultured rat DRG neurones.

物理化学性质&存储条件

分子量 518.459
分子式 C27H20F6N2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4,4'-(Hexafluoroisopropylidene)bis(p-phenyleneoxy)dianiline

参考文献

1. Loucif AJC, et al. Br J Pharmacol. 2017 Nov 18. doi: 10.1111/bph.14098.

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