GI 530159 是 TREK1 和 TREK2 钾通道的选择性开放剂。
货号:ajcx27770
CAS:69563-88-8
分子式:C27H20F6N2O2
分子量：518.45
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro.

Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID:29150838