半岛bd体育手机客户端 说明
一般描述
An aminobenzimidazole derivative that selectively and reversibly blocks small conductance Ca2+-activated K+ channels (SK1-3; Kd= 420 nM, 600 nM, and 730 nM for SK1, SK2, SK3, respectively) in a Ca2+-dependent manner. It mediates channel gating by interacting with gating structures deep within the inner pore vestibule where Ser507 and Ala532 are deemed to be important for inhibition. Interacts at a site that is distinct from the apamin binding site in SK channels. Can access high-affinity binding sites from both the inside and outside of the cell membrane. Does not affect QT intervals, but prolongs the atrial effective refractive period and prevents acetylcholine-induced atrial fibrillations inex vivoandin vivomodels. Also shown to reversibly block TRPM7 channel (IC50= 1.6 mM) in smooth muscle cells, primary podocytes, HEK293 cells expressing TRPM7, and ventricular myocytes in a Mg2+-dependent manner and blocks the motility of cells in culture.
包装
10 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Chubanov, V., et al. 2012.Brit. Journ. Pharm.166,1357.
Jenkins, D., et al. 2011.Hypertension.57,1129.
Jenkins, D., et al. 2011.Mol. Pharm.79,899.
Jenkins, D., et al. 2011.Mol. Pharm.79,899.
Lasse, S., et al. 2011.J. Cardiov. Pharm.57,672.
Diness, J., et al. 2010.Circ Arrhythm Electrophusiol.3,380.
Ji, H., et al. 2009.Eur. J. Neurosci.9,1883.
Strobaek, D., et al. 2006.Mol. Pharm.70,1771.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C17H17N3 |
分子量 | 263.34 |
MDL编号 | MFCD32671885 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | white |
溶解性 | DMSO: 100 mg/mL |
运输 | wet ice |
储存温度 | 2-8℃ |
SMILES string | C1(NC(N[C@@H]2CCCC3=C2C=CC=C3)=N4)=C4C=CC=C1 |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
Sigma-Aldrich