101526-62-9
101526-62-9 结构式
基本信息
中文别名
司美利特盐酸盐司美利特盐酸盐一水合物
SEMATILIDE 单盐酸盐 一水合物
N-[2-(DIETHYLAMINO)ETHYL]-4′-[(METHYLSULFONYL)AMINO]BENZAMIDE 单盐酸盐 一水合物
英文别名
CK-1752Ck 1752a
Sematilide HCl
Sematilide (CK-1752)
Sematilide hydrochloride
Sematilide monohydrochloride
Sematilide monohydrochloride monohydrate
Sematilide monohydrate monohydrochloride
N-[2-(diethylamino)ethyl]-4-(methanesulfonamido)benzamide,hydrochloride
N-(2-(Diethylamino)ethyl)-4-((methylsulfonyl)amino)benzamide monohydrochloride
物理化学性质
熔点141-142° (Lumma); mp 137° and mp 142° (Argentieri)
储存条件2-8°C
溶解度在水中的溶解度≥16mg/mL
酸度系数(pKa)pKa1 7.60; pKa2 9.51(at 25℃)
形态粉末
颜色白色至米色
安全数据
WGK Germany3
毒性LD50 i.p. in mice: 250-300 mg/kg (Lumma); LD50 in mice, rats, dogs (mg/kg): 96, 92, 143-175 i.v.; 1,800, 3,200, 500-1,000 orally (Argentieri)
常见问题列表
生物活性
Sematilide hydrochloride (CK-1752 hydrochloride) 是一种选择性的 IKr 通道阻滞剂。Sematilide 抑制延迟整流钾通道 (K+ current)，IC50 为 25 μM，这种作用存在浓度依赖性。Sematilide 是一种 III 类抗心律不齐剂。靶点
IC50: 25 μM (K + current)
体外研究
Application of 10, 30, 100 and 300 μM Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC 50 =25 μM).
体内研究
Sematilide (0.3-1.0 mg/kg, intravenously i.v.) is effective in a canine model of arrhythmia.
| Animal Model: | Mongrel dogs of either sex (10-18 kg body weight) |
| Dosage: | 0.3, 1, 3, and 10 mg/kg |
| Administration: | I.v. infusions |
| Result: | Demonstrated antiarrhythmic effects at 0.3 and 3.0 mg/kg. |