GI 530159 是 TREK1 和 TREK2 钾通道的选择性开放剂。
Cas No. | 69563-88-8 |
别名 | 2,2-双[4-(4-氨基苯氧基)苯基]-1,1,1,3,3,3-六氟丙烷 |
Canonical SMILES | NC1=CC=C(C=C1)OC2=CC=C(C(C(F)(F)F)(C(F)(F)F)C3=CC=C(C=C3)OC4=CC=C(C=C4)N)C=C2 |
分子式 | C27H20F6N2O2 |
分子量 | 518.45 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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 |