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Submit ReviewML 365 is a potent and selective TASK-1 (K2P3.1/KCNK3) channel blocker (IC50 values are 4 and 390 nM at TASK-1 and TASK-3, respectively). Displays little or no inhibition at Kir2.1, voltage-gated potassium channels, KCNQ2 and KV11.1 (hERG).
ML 365 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 360.41 |
公式 | C22H20N2O3 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 947914-18-3 |
PubChem ID | 46785920 |
InChI Key | UTAJHKSGYJSZBR-UHFFFAOYSA-N |
Smiles | CC1=CC=CC(C(NC2=CC(NC(C3=CC=CC=C3OC)=O)=CC=C2)=O)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.04 | 100 | |
ethanol | 18.02 | 50 |
以下数据基于产品分子量 360.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.77 mL | 13.87 mL | 27.75 mL |
5 mM | 0.55 mL | 2.77 mL | 5.55 mL |
10 mM | 0.28 mL | 1.39 mL | 2.77 mL |
50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Flaherty et al (2014) Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold. Bioorg.Med.Chem.Lett. 24 3968 PMID: 25017033
Zou et al (2013) ML365: Development of bis-amides as selective inhibitors of the KCNK3/TASK1 two pore potassium channel. Probe Reports from the NIH Molecular Libraries Program PMID: 24479195
If you know of a relevant reference for ML 365, please let us know.
关键词: ML 365, ML 365 supplier, ML365, Potassium, channels, subfamily, K, member, 3, k2p3.1, KCNK3, potent, selective, TASK1, inhibitors, inhibits, TASK3, TWIK, related, acid, sensitive, K+, two, pore, potassium, channel, Two-P, Channels, 5337, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 ML 365 的部分引用包括:
Vierra et al (2017) TALK-1 channels control β cell endoplasmic reticulum Ca2+ homeostasis. Sci Signal 10 PMID: 28928238
Richard L et al (2021) Modulation of TASK-1/3 channels at the hypoglossal motoneuron pool and effects on tongue motor output and responses to excitatory inputs in vivo: implications for strategies for obstructive sleep apnea pharmacotherapy. Sleep 44 PMID: 32745213
Pagani et al (2019) How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch. Neuron PMID: 31103358
Veldkamp et al (2018) Neurokinin-3 receptor activation selectively prolongs atrial refractoriness by inhibition of a background K+ channel. Nat. Commun. 9 4357 PMID: 30341287
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平均评分: 5 (Based on 1 Review.)
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This product was used to study the channel blocking activity on K2p1.1 channels. It was identified that it shows certain degree of channel blocking although that is not concentration dependent. Would buy again as the results obtained were reproducible at every trial study.