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E-4031是甲磺酰苯胺III 类抗心律失常药,选择性地阻断hERG 钾通道。
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E-4031是甲磺酰苯胺III 类抗心律失常药,选择性地阻断hERG 钾通道。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 262 | 现货 | |
2 mg | ¥ 369 | 现货 | |
5 mg | ¥ 545 | 现货 | |
10 mg | ¥ 971 | 现货 | |
25 mg | ¥ 1,920 | 现货 | |
50 mg | ¥ 2,950 | 现货 | |
100 mg | ¥ 4,350 | 现货 |
产品描述 | E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM) |
靶点活性 | ERG K+ channel (human):29 nM |
体内活性 | 在基线条件下,LQT1兔在左室(LV)顶端和右室(RV)中部的APD较LMC兔更长。红霉素和E-4031在所有位置都延长了LQT1和LMC兔的APD。然而,红霉素引起的基于基线的APD延长百分比(%APD)在LQT1的LV基底侧和RV中部位置更为明显(100 μM, LQT1, +40.6 ± 9.7% 对比 LMC, +24.1 ± 10.0%, p<0.05),而E-4031引起的%APD延长在LQT1的LV基底侧(0.01 μM, LQT1, +29.6 ± 10.6% 对比 LMC, +19.1 ± 3.8%, p<0.05)和LV基底隔膜位置更为显著。此外,红霉素在LQT1中显著增加了空间APD分散,并且仅在LQT1的LV基底隔膜和RV中部位置增加了三角化。类似地,E-4031仅在LQT1的LV顶端和基底隔膜位置增加了三角化。 |
动物实验 | Hearts of adult female transgenic LQT1 and wild type littermate control (LMC) rabbits were Langendorff-perfused with increasing concentrations of HERG/IKr-blockers E-4031 (0.001-0.1 μM, n=9/7) and APD, APD dispersion, and triangulation were analyzed[1]. |
别名 | (1S)-1,5-脱水-1-C-[4-氯-3-[[4-[2-(环丙氧基)乙氧基]苯基]甲基]苯基]-D-山梨醇 |
分子量 | 474.44 |
分子式 | C21H29Cl2N3O3S |
CAS No. | 113559-13-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 50 mg/mL (105.39 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
H2O
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