货号 | 15193-1mg |
描述 | Potassium (K+) channels are categorized by their mode of activation and the number of transmembrane segments.1 The voltage-gated six-transmembrane K+ channels include KCNQ1, first recognized for its role in cardiac function and subsequently in hearing, gastrointestinal chloride secretion, and other processes.1,2 ML-277 is a potent activator of KCNQ1 channels (EC50 = 260 nM).3 The EC50 value of this compound at the related channels KCNQ2, KCNQ4, and hERG exceeds 30 µM.3 ML-277 potentiates both homomultimeric KCNQ1 channels and unsaturated heteromultimeric (KCNQ1/KCNE1) channels in model cardiomyocytes and augments delayed rectifier K+ current in cultured human cardiomyocytes.4 |
别名 | CID-53347902; |
供应商 | Cayman |
应用文献 | |
1.Wulff, H.,Castle, N.A. and Pardo, L.A. Voltage-gated potassium channels as therapeutic targets. Nature Reviews.Drug Discovery 8(12), 982-1001 (2009). 2.Robbins, J. KCNQ potassium channels: Physiology, pathophysiology, and pharmacology. Pharmacology & Therapeutics 90(1), 1-19 (2001). 3.Mattmann, M.E.,Yu, H.,Lin, Z., et al. Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator. Bioorganic & Medicinal Chemistry Letters 22(18), 5936-5941 (2012). 4.Yu, H.,Lin, Z.,Mattmann, M.E., et al. Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels. Proceedings of the National Academy of Sciences of the United States of America 110(21), 8732-8737 (2013). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 471.6 |
分子式 | C23H25N3O4S2 |
CAS号 | 1401242-74-7 |
稳定性 | ≥ 2 years |
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