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Catalog: | HY-W013712 |
Brand: | MCE |
CAS: | 69563-88-8 |
MDL | MFCD00015723 |
---|---|
Molecular Weight | 518.45 |
Molecular Formula | C27H20F6N2O2 |
SMILES | FC(C(C1=CC=C(OC2=CC=C(N)C=C2)C=C1)(C3=CC=C(OC4=CC=C(N)C=C4)C=C3)C(F)(F)F)(F)F |
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 [1] .
Target: TREK1/2 [1]
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 EC
50
s 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 250 mg/mL ( 482.21 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.9288 mL | 9.6441 mL | 19.2883 mL |
5 mM | 0.3858 mL | 1.9288 mL | 3.8577 mL |
10 mM | 0.1929 mL | 0.9644 mL | 1.9288 mL |
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