ML-297 (Synonyms: CID-56642816,VU0456810) |
| رقم الكتالوجGC15117 |
ML-297 (VU 0456810) هو منشط قوي وانتقائي GIRK1 / 2 ، مع EC50 من 0.16 ميكرومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1443246-62-5
Sample solution is provided at 25 µL, 10mM.
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EC50: 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4, respectively.
ML-297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator.
G protein-regulated inwardly rectifying potassium (GIRK1-4) channels are a family of Kir3.1-Kir3.4 ion channels modulating cell excitability. The four different GIRK subunits are composed in different combinations expressed with regional specificity throughout the central nervous system and in the periphery.
In vitro: In thallium flux assays, ML297 showed concentration-dependent efficacy when tested on cells expressing GIRK1/2. ML297 could also activate GIRK channels comprised of GIRK1/3 and GIRK1/4 subunit combinations. However, ML297 diaplayed a complete inability to modulate the activity of HEK-293 cells expressing GIRK2 alone. A similar complete lack of efficacy was seen when ML297 was tested on HEK-293 cells expressing GIRK2/3. Therefore, it appeared that ML297 is only capable of activating GIRK channels containing a GIRK1 subunit [1].
In vivo: Previous study performed an ascending dose study in mice and it was found that the animals appeared normal and not under obvious distress at all doses tested. ML297’s effects on locomotor activity as well as effects on motor function and coordination were further evaluated. Results showed that ML297 at 60 mg/kg could immediate decrease in locomotor activity compared to the control group [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Kaufmann, K. ,Romaine, I.M.,Days, E., et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem.Neurosci. 4(9), 1278-1286 (2013).
| Cas No. | 1443246-62-5 | SDF | |
| المرادفات | CID-56642816,VU0456810 | ||
| Chemical Name | N-(3,4-difluorophenyl)-N'-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-urea | ||
| Canonical SMILES | O=C(NC1=CC(F)=C(F)C=C1)NC2=CC(C)=NN2C3=CC=CC=C3 | ||
| Formula | C17H14F2N4O | M.Wt | 328.3 |
| الذوبان | ≤20mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.046 mL | 15.23 mL | 30.4599 mL |
| 5 mM | 609.2 μL | 3.046 mL | 6.092 mL |
| 10 mM | 304.6 μL | 1.523 mL | 3.046 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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