| 货号 | 18608-1mg |
| 描述 | Zatebradine is a bradycardic compound that blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells (IC50s = 1.83, 2.21, 1.9, and 1.88 µM, respectively for HCN1-4 in vitro).1,2 Additionally, it can block voltage-gated outward K+(IK) currents and related neuronal hyperpolarization-activated inward current (Ih) channels, but exhibits little or no activity for L-type Ca2+(ICa) currents.3,4 When assessed through telemetric ECG recording in mice, zatebradine reduced heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induced increasing arrhythmia at concentrations >10 mg/kg.1 |
| 别名 | UL-FS 49; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Stieber, J.,Wieland, K.,Stöckl, G., et al. Bradycardic and proarrhythmic properties of sinus node inhibitors. Molecular Pharmacology 69(4), 1328-1337 (2006). 2.Melchiorre, M.,Del Lungo, M.,Guandalini, L., et al. Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers. Journal of Medicinal Chemistry 53(18), 6773-6777 (2010). 3.Satoh, T.O., and Yamada, M. Multiple inhibitory effects of zatebradine (UL-FS 49) on the electrophysiological properties of retinal rod photoreceptors. Pflugers.Arch. 443(4), 532-540 (2002). 4.BoSmith, R.E.,Briggs, I., and Sturgess, N.C. Inhibitory actions of ZENECA ZD7288 on whole-cell hyperpolarization activated inward current (If) in guinea-pig dissociated sinoatrial node cells. British Journal of Pharmacology 110(1), 343-349 (1993). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 493 |
| 分子式 | C26H36N2O5 • HCl |
| CAS号 | 91940-87-3 |
| 稳定性 | ≥ 2 years |
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