CK-1752

CK-1752用途

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。

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CK-1752名称

[ CAS 号 ]:
101526-62-9

[ 中文名 ]:
司美利特

[ 英文名 ]:
Sematilide hydrochloride

[英文别名 ]:

Sematilide HCl
SEMATILIDE HYDROCHLORIDE
CK 1752A
Sematilide hydrochloride (USAN)
Sematilide monohydrochloride
[14C]-Sematilide hydrochloride

CK-1752生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

IC50: 25 μM (K+ current)[1]

[体外研究]

应用10μM、30μM、100μM和300μM三聚体可引起延迟整流K+电流(IC50=25μM)的浓度依赖性抑制[1]。

[体内研究]

Sematile(0.3-1.0 mg/kg,静脉注射)对犬心律失常模型有效[2]。动物模型：雌雄各半的杂种狗(体重10-18公斤)[2]剂量：0.3、1、3和10毫克/公斤给药：静脉滴注结果：0.3和3.0毫克/公斤有抗心律失常作用。

[参考文献]

[1]. Ishii Y, et al. Effects of Sematilide, a novel class III antiarrhythmic agent, on membrane currents in rabbit atrial myocytes. Eur J Pharmacol. 1997 Jul 23;331(2-3):295-302.

[2]. Stanley S. Greenberg, et al. Pharmacology of Sematilide, a non-quaternary class III antiarrhythmic agent.

CK-1752物理化学性质

[ 沸点 ]:
511.9ºC at 760 mmHg

[ 分子式 ]:
C₁₄H₂₄ClN₃O₃S

[ 分子量 ]:
349.87700

[ 闪点 ]:
263.4ºC

[ 精确质量 ]:
349.12300

[ PSA ]:
86.89000

[ LogP ]:
3.47640

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
7.59E-11mmHg at 25°C

[ 储存条件 ]:
-20℃

CK-1752MSDS

详细MSDS(安全技术说明书)

CK-1752毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CV4203840

CHEMICAL NAME :: Benzamide, N-(2-(diethylamino)ethyl)-4-((methylsulfonyl)amino)-, monohydrochloride

CAS REGISTRY NUMBER :: 101526-62-9

LAST UPDATED :: 199603

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C14-H23-N3-O3-S.Cl-H

MOLECULAR WEIGHT :: 349.92

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3200 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 92 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1800 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 96 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 143 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 90 gm/kg/90D-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 27 gm/kg/90D-I

TOXIC EFFECTS :: Behavioral - ataxia Gastrointestinal - nausea or vomiting Related to Chronic Data - death

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992