| CAS NO: | 133229-11-5 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | White solid |
| Storage | Store at RT |
| M.Wt | 483.84 |
| Cas No. | 133229-11-5 |
| Formula | C19H24Cl2N2O4S·HCl |
| Solubility | <48.38mg/ml in DMSO;<24.19mg/ml in H2O |
| Chemical Name | N-(4-(3-((3,4-dichlorophenethyl)(methyl)amino)-2-hydroxypropoxy)phenyl)methanesulfonamide hydrochloride |
| Canonical SMILES | CN(CC(O)COC1=CC=C(NS(C)(=O)=O)C=C1)CCC2=CC(Cl)=C(Cl)C=C2.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
AM 92016 hydrochloride是一种特异性的延迟整流钾电流抑制剂[1].
钾通道是一种离子通道,用于复位静息电位和形成动作电位.延迟整流钾通道(IK)由Na+流入和K +排出激活,将膜去极化.IK限制神经冲动的持续时间.
AM 92016 hydrochloride是一种特异性的iK抑制剂.在豚鼠和兔心室肌细胞中,AM 92016显著增加动作电位时程,复极水平分别为20％和90％.此外,AM 92016(1 μM)时间依赖性地抑制去极化激活的IK [1].在兔窦房结细胞中,AM 92016(50 nM)浓度依赖性地显著抑制IK,IC50值为40 nM [2].在血管平滑肌细胞(VSMC)中,AM 92016 hydrochloride抑制NO诱导的ERK1/2去磷酸化[3].
在豚鼠中,AM 92016(1-5 mg/kg)显著增加心率\左室收缩压\动脉收缩压和收缩指数dp dtmax.AM 92016表现出心律失常活动[4].
参考文献：
[1]. Connors SP, Gill EW, Terrar DA. Actions and mechanisms of action of novel analogues of sotalol on guinea-pig and rabbit ventricular cells. Br J Pharmacol, 1992, 106(4): 958-965.
[2]. Lei M, Brown HF. Inhibition by Compound II, a sotalol analogue, of delayed rectifier current (iK) in rabbit isolated sino-atrial node cells. Naunyn Schmiedebergs Arch Pharmacol, 1998, 357(3): 260-267.
[3]. Palen DI, Belmadani S, Lucchesi PA, et al. Role of SHP-1, Kv.1.2, and cGMP in nitric oxide-induced ERK1/2 MAP kinase dephosphorylation in rat vascular smooth muscle cells. Cardiovasc Res, 2005, 68(2): 268-277.
[4]. Hagerty MJ, Wainwright CL, Kane KA. The in-vivo cardiovascular effects of a putative class III anti-arrhythmic drug, AM 92016. J Pharm Pharmacol, 1996, 48(4): 417-421.
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