ML 297
Based on 2 publication(s) in Google Scholar
ML 297 (VU 0456810) is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM. ML 297 can cross the blood-brain barrier with brain-to-plasma ratio of 0.2 in mice model (i.p.). ML 297 is potential for the treatment of epilepsy.
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- Purity: 99.14%
- CAS No.: 1443246-62-5
- 화학식: C17H14F2N4O
- 분자량:328.32
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML 297
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Biological Activity
EC50: 0.16 μM (GIRK1/2), 18 μM (GIRK1/4)[1]
ML 297 is completely inactive for GIRK2/3[1].
ML297 shows concentration-dependent efficacy in expressing GIRK1/2 cells and with an EC50 of 162 nM[2].
ML297 shows a complete inability to modulate the activity of HEK-293 cells expressing GIRK2 alone and GIRKGIRK2/3[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ML297 (60 mg/kg; ip) shows a maximal free plasma concentration (Cmax) of 640 nM with a corresponding free brain Cmax of 130 nM, producing a brain-to-plasma ratio of 0.2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8-10 months old C57/BL6 male mice (approximately 30 g)[2]
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Dosage:60 mg/kg
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Administration:Intraperitoneal injection
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Result:Most of the animals neither convulsions nor death.
Chemical Information
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CAS No. 1443246-62-5
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Appearance Solid
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분자량 328.32
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화학식 C17H14F2N4O
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Color White to off-white
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SMILES
FC1=C(F)C=CC(NC(NC2=CC(C)=NN2C3=CC=CC=C3)=O)=C1
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Synonyms
VU 0456810; CID 56642816
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
2026 Jun 19. PMID: 42321470 -
용액&용해도
DMSO : 250 mg/mL (761.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Korean - KR (458 KB)
- Portuguese - PT (458 KB)
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Handling Instructions (2659 KB)
References
[1]. Wen W, et al. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4562-6. [Content Brief]
[2]. Kaufmann K, et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0458 mL | 15.2290 mL | 30.4581 mL | 76.1452 mL |
| 5 mM | 0.6092 mL | 3.0458 mL | 6.0916 mL | 15.2290 mL | |
| 10 mM | 0.3046 mL | 1.5229 mL | 3.0458 mL | 7.6145 mL | |
| 15 mM | 0.2031 mL | 1.0153 mL | 2.0305 mL | 5.0763 mL | |
| 20 mM | 0.1523 mL | 0.7615 mL | 1.5229 mL | 3.8073 mL | |
| 25 mM | 0.1218 mL | 0.6092 mL | 1.2183 mL | 3.0458 mL | |
| 30 mM | 0.1015 mL | 0.5076 mL | 1.0153 mL | 2.5382 mL | |
| 40 mM | 0.0761 mL | 0.3807 mL | 0.7615 mL | 1.9036 mL | |
| 50 mM | 0.0609 mL | 0.3046 mL | 0.6092 mL | 1.5229 mL | |
| 60 mM | 0.0508 mL | 0.2538 mL | 0.5076 mL | 1.2691 mL | |
| 80 mM | 0.0381 mL | 0.1904 mL | 0.3807 mL | 0.9518 mL | |
| 100 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7615 mL |
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