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Submit ReviewML 252 is a potent and selective inhibitor of KV7.2 voltage-gated potassium channels (IC50 = 70 nM), which displays >40-fold selectivity for KV7.2 over KV7.1 channels (IC50 = 2.9 μM for KV7.1). ML 252 is the (S)-enantiomer, and is more potent than the (R)-enantiomer or racemic mixture (IC50 values are 944 and 160 nM, respectively). ML 252 displays selectivity for KV7.2 over a panel of >68 GPCRs, ion channels and transporters; inhibits melatonin MT1 receptor 60% at 10 μM. ML 252 is brain penetrant.
ML 252 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 | 308.43 |
公式 | C20H24N2O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1392494-64-2 |
PubChem ID | 26873419 |
InChI Key | FROGGFONBYACJB-UHFFFAOYSA-N |
Smiles | O=C([C@@H](CC)C1=CC=CC=C1)NC2=C(N3CCCC3)C=CC=C2 |
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 | 30.84 | 100 | |
ethanol | 30.84 | 100 |
以下数据基于产品分子量 308.43。 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 | 3.24 mL | 16.21 mL | 32.42 mL |
5 mM | 0.65 mL | 3.24 mL | 6.48 mL |
10 mM | 0.32 mL | 1.62 mL | 3.24 mL |
50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
参考文献是支持产品生物活性的出版物。
Cheung et al (2012) Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of KV7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phe J.Med.Chem. 55 6975 PMID: 22793372
If you know of a relevant reference for ML 252, please let us know.
关键词: ML 252, ML 252 supplier, ML252, voltage, gated, potassium, channel, Kv7.2, inhibitor, inhibits, potent, brain, penetrant, selective, Voltage-Gated, Potassium, Channels, 4687, Tocris Bioscience
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