| Field | Specification |
|---|---|
| Alternative names | VU 0456810; CID 56642816 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C17H14F2N4O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
ML 297, also known as VU 0456810 or CID 56642816, is a potent, selective GIRK1/2 activator with an EC50 of 0.16 μM. It can cross the blood-brain barrier, with a brain-to-plasma ratio of 0.2 in a mouse model (i.p.), and has been studied for potential use in epilepsy treatment[1][2]. It is supplied as a white to off-white solid (C17H14F2N4O, MW 328.32) at 99.14% purity.
Physical & Chemical Properties
| CAS Number | 1443246-62-5 |
|---|---|
| Molecular Formula | C17H14F2N4O |
| Molecular Weight | 328.32 g/mol |
| Purity | 99.14% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | FC1=C(F)C=CC(NC(NC2=CC(C)=NN2C3=CC=CC=C3)=O)=C1 |
| Signaling Pathway | Membrane Transporter/Ion Channel |
| Solubility | In Vitro: DMSO: 250 mg/mL (761.45 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
EC50: 0.16 μM (GIRK1/2), 18 μM (GIRK1/4)[1]
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 | 250 mg/mL (761.45 mM) | requires sonication; 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 + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (6.34 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (6.34 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 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 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (6.34 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 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 (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
ML 297 has no activity at all at GIRK2/3[1]. ML297 is efficacious in a concentration-dependent manner in cells expressing GIRK1/2, with an EC50 of 162 nM[2]. ML297 is entirely unable to modulate the activity of HEK-293 cells expressing GIRK2 alone or GIRK2/3[2].
In Vivo
ML297 (60 mg/kg; i.p.) highly significantly prevents both convulsions and fatality caused by treatment with the GABAA antagonist pentylenetetrazol (PTZ)[2]. ML297 (60 mg/kg; ip) gives a maximal free plasma concentration (Cmax) of 640 nM and a matching free brain Cmax of 130 nM, for a brain-to-plasma ratio of 0.2[2].
| Animal Model | 8-10 months old C57/BL6 male mice (approximately 30 g)[2] |
|---|---|
| Dosage | 60 mg/kg |
| Administration | Intraperitoneal injection |
| Result | Most of the animals neither convulsions nor death. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Tryptamine from wake-active monoaminergic neurons regulates sleep homeostasis. Nat Neurosci 2026 Jun 19. PMID: 42321470
Research Square Preprint. 2020 Dec.
