101526-62-9
101526-62-9 結(jié)構(gòu)式
基本信息
中文別名
司美利特鹽酸鹽司美利特鹽酸鹽一水合物
SEMATILIDE 單鹽酸鹽 一水合物
N-[2-(DIETHYLAMINO)ETHYL]-4′-[(METHYLSULFONYL)AMINO]BENZAMIDE 單鹽酸鹽 一水合物
英文別名
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
物理化學(xué)性質(zhì)
熔點(diǎn)141-142° (Lumma); mp 137° and mp 142° (Argentieri)
儲(chǔ)存條件2-8°C
溶解度在水中的溶解度≥16mg/mL
酸度系數(shù)(pKa)pKa1 7.60; pKa2 9.51(at 25℃)
形態(tài)粉末
顏色白色至米色
安全數(shù)據(jù)
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)
常見問題列表
生物活性
Sematilide hydrochloride (CK-1752 hydrochloride) 是一種選擇性的 IKr 通道阻滯劑。Sematilide 抑制延遲整流鉀通道 (K+ current)，IC50 為 25 μM，這種作用存在濃度依賴性。Sematilide 是一種 III 類抗心律不齊劑。靶點(diǎn)
IC50: 25 μM (K + current)
體外研究
Application of 10, 30, 100 and 300 μM Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC 50 =25 μM).
體內(nèi)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. |