ML277
Based on 2 publication(s) in Google Scholar
ML277 (CID-53347902) is a potent and selective activator of K(v)7.1 (KCNQ1) potassium channel activator (EC50=270 nM), rescues function of pathophysiologically important mutant channel complexes in human induced pluripotent stem cell-derived cardiomyocytes.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.46%
- CAS 番号: 1401242-74-7
- 分子式: C23H25N3O4S2
- 分子量:471.59
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 ML277
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>30 μM
Compound: 10c, ML277, VU0458298, CID 53347902
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Activation of KCNQ2 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay relative to control
Activation of KCNQ2 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay relative to control
|
[PMID: 22910039] |
| CHO | EC50 |
>30 μM
Compound: 10c, ML277, VU0458298, CID 53347902
|
Activation of KCNQ4 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay relative to control
Activation of KCNQ4 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay relative to control
|
[PMID: 22910039] |
| CHO | EC50 |
0.26 μM
Compound: 10c, ML277, VU0458298, CID 53347902
|
Activation of Kv7.1 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay
Activation of Kv7.1 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay
|
[PMID: 22910039] |
| CHO | IC50 |
>30 μM
Compound: 10c, ML277, VU0458298, CID 53347902
|
Inhibition of human ERG expressed in CHO cells after 3 mins by patch clamp assay
Inhibition of human ERG expressed in CHO cells after 3 mins by patch clamp assay
|
[PMID: 22910039] |
体外実験
ML277 (1 μM) increases the amplitude of KCNQ1 whole-cell and single-channel currents[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
化学情報
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CAS 番号 1401242-74-7
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性状 Solid
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分子量 471.59
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分子式 C23H25N3O4S2
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Color White to off-white
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SMILES
O=C([C@@H]1N(S(=O)(C2=CC=C(C)C=C2)=O)CCCC1)NC3=NC(C4=CC=C(OC)C=C4)=CS3
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別名
CID-53347902
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Am J Physiol Cell Physiol
M2 muscarinic receptor-dependent contractions of airway smooth muscle are mediated by inhibition of Kv7 channels. [Abstract]2026 Mar 5. PMID: 41784087 -
溶剤 & 溶解度
体外:
DMSO : ≥ 56 mg/mL (118.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
In Vivo Dissolution Calculator
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.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Eldstrom J, et al. ML277 regulates KCNQ1 single-channel amplitudes and kinetics, modified by voltage sensor state. J Gen Physiol. 2021 Dec 6;153(12):e202112969. [Content Brief]
[2]. Mattmann ME, et al. Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5936-41. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1205 mL | 10.6024 mL | 21.2049 mL | 53.0122 mL |
| 5 mM | 0.4241 mL | 2.1205 mL | 4.2410 mL | 10.6024 mL | |
| 10 mM | 0.2120 mL | 1.0602 mL | 2.1205 mL | 5.3012 mL | |
| 15 mM | 0.1414 mL | 0.7068 mL | 1.4137 mL | 3.5341 mL | |
| 20 mM | 0.1060 mL | 0.5301 mL | 1.0602 mL | 2.6506 mL | |
| 25 mM | 0.0848 mL | 0.4241 mL | 0.8482 mL | 2.1205 mL | |
| 30 mM | 0.0707 mL | 0.3534 mL | 0.7068 mL | 1.7671 mL | |
| 40 mM | 0.0530 mL | 0.2651 mL | 0.5301 mL | 1.3253 mL | |
| 50 mM | 0.0424 mL | 0.2120 mL | 0.4241 mL | 1.0602 mL | |
| 60 mM | 0.0353 mL | 0.1767 mL | 0.3534 mL | 0.8835 mL | |
| 80 mM | 0.0265 mL | 0.1325 mL | 0.2651 mL | 0.6627 mL | |
| 100 mM | 0.0212 mL | 0.1060 mL | 0.2120 mL | 0.5301 mL |