| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H20F6N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GI-530159 selectively opens the TREK1 and TREK2 potassium channels, showing selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels with an EC50 of 0.76 μM at TREK1. It reduces excitability of rat dorsal root ganglion neurons and shows a potential analgesic effect[1]. It is supplied as a white to off-white solid (C27H20F6N2O2, MW 518.45) at 99.45% purity.
Physical & Chemical Properties
| CAS Number | 69563-88-8 |
|---|---|
| Molecular Formula | C27H20F6N2O2 |
| Molecular Weight | 518.45 g/mol |
| Purity | 99.45% |
| Appearance | Solid |
| Color | White to off-white |
| 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 |
| Signaling Pathway | Membrane Transporter/Ion Channel |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (192.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (192.88 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 5 mg/mL (9.64 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (9.64 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
TREK (TWIK-related K) two pore domain potassium (K2P) channels mediate pain perception and control the excitability of somatosensory nociceptive neurons[1]. GI-530159 (1 μM or 10 μM) is selective, activating TREK1 and TREK2 channels without significant effects on TRAAK channels or the K channels tested[1]. GI-530159 (0.1-30 μM) activates recombinant human TREK1 channels, with EC50s of 0.8 μM from Rb efflux and 0.9 μM from electrophysiological experiments[1]. In rat dorsal root ganglion (DRG) neurons, GI-530159 (1 μM) reduces excitability, lowering firing frequency and slightly hyperpolarizing the resting membrane potential (RMP)[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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