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Purity: ≥98%
ML365 is a potent, novel and selective small molecule inhibitor of the TASK1(KCNK3, a two-pore domain potassium channel). ML365 blocks TASK1 channels in both the thallium influx fluorescent assay (IC50 = 4 nM) and an automated electrophysiology assay (IC50 = 16 nM). Based on potency differences, it possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related, two-pore domain potassium channel, TASK3. ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). Based on these criteria, ML365 is a best-in-class probe and is a useful pharmacological probe for in vitro studies of TASK1 function and in further studies aimed at developing therapeutic intervention.
| ln Vitro |
In automated electrophysiological studies (IC50 = 16 nM) and thallium influx fluorescence assays (IC50 = 4 nM), ML365 inhibits TASK1 channels [1]. At 30 μM or no inhibitory impact, ML365 has minimal activity against the potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), human ether-a go-go related gene (hERG), and the distantly related potassium channel Kir2.1 [1]. ML365 does not show acute toxicity in cell-based studies at doses as high as 30 μM [1].
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| References |
| Molecular Formula |
C22H20N2O3
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| Molecular Weight |
360.41
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| Exact Mass |
360.147
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| CAS # |
947914-18-3
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| Related CAS # |
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| PubChem CID |
46785920
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| Appearance |
White to off-white solid powder
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| Density |
1.253±0.06 g/cm3 (20 °C, 760 mmHg)
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| Boiling Point |
429.9±40.0 °C (760 mmHg)
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| LogP |
4.654
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UTAJHKSGYJSZBR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20N2O3/c1-15-7-5-8-16(13-15)21(25)23-17-9-6-10-18(14-17)24-22(26)19-11-3-4-12-20(19)27-2/h3-14H,1-2H3,(H,23,25)(H,24,26)
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL | |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Control experiment with ethacrynic acid (panel A) and chemical stability of ML365 over 8 h in the presence of a 5-fold concentration of dithiothreitol (panel B).PMID: 24479195 |
Inhibition of thallium signal in TASK1/KCNK3-expressing cells by ML365.
Selectivity of ML365 effect against various potassium channels using fluorescent-based assays.PMID: 24479195 |
Aqueous stability of ML365 over 48 h in 1:1 PBS/acetonitrile.
Selectivity of ML365 effect for TASK1 as compared to TASK3 using QPatch 16X.PMID: 24479195 |
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