GI 530159

Pricing Availability   Qty
Description: K2P2.1 (TREK-1) and K2P10.1 (TREK-2) channel activator
Chemical Name: 4,4'-[[2,2,2-Trifluoro-1-(trifluoromethyl)ethylidene]bis(4,1-phenyleneoxy)]bis[benzenamine]
Purity: ≥99% (HPLC)

Biological Activity for GI 530159

GI 530159 is a 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.

Compound Libraries for GI 530159

GI 530159 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GI 530159

M. Wt 518.45
Formula C27H20F6N2O2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 69563-88-8
PubChem ID 94652
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 for GI 530159

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

Preparing Stock Solutions for GI 530159

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.

Select a batch to recalculate based on the batch molecular weight:
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 for GI 530159

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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Citations for GI 530159

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