| Bioactivity | 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[1]. | ||||||||||||
| Target | Target: TREK1/2 | ||||||||||||
| Invitro | TREK (TWIK-related K) two pore domain potassium (K2P) channels regulate the excitability of somatosensory nociceptive neurons and mediate pain perception[1].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[1].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[1].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)[1]. | ||||||||||||
| Name | GI-530159 | ||||||||||||
| CAS | 69563-88-8 | ||||||||||||
| Formula | C27H20F6N2O2 | ||||||||||||
| Molar Mass | 518.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
GI-530159
CAS: 69563-88-8 F: C27H20F6N2O2 W: 518.45
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over T
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