GI 530159

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Cat.No. 6689 - GI 530159 | C27H20F6N2O2 | CAS No. 69563-88-8
Description: TREK1 and TREK2 channel activator
Chemical Name: 4,4'-[[2,2,2-Trifluoro-1-(trifluoromethyl)ethylidene]bis(4,1-phenyleneoxy)]bis[benzenamine]
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

M. Wt 518.45
Formula C27H20F6N2O2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 69563-88-8
PubChem ID 94652
InChI Key HHLMWQDRYZAENA-UHFFFAOYSA-N
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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.84 100
ethanol 25.92 50

Preparing Stock Solutions

The following data is based on the product molecular weight 518.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.93 mL 9.64 mL 19.29 mL
5 mM 0.39 mL 1.93 mL 3.86 mL
10 mM 0.19 mL 0.96 mL 1.93 mL
50 mM 0.04 mL 0.19 mL 0.39 mL

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References

References are publications that support the biological activity of the product.

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


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