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氯非铵甲苯磺酸盐

氯非铵甲苯磺酸盐用途

Clofilium tosylate 是一种钾通道 (potassium channel) 阻滞剂,作用于人早幼粒细胞白血病 (HL-60) 细胞,激活 caspase-3 而诱导凋亡。具有抗心律失常作用。

氯非铵甲苯磺酸盐名称

[ CAS 号 ]:
92953-10-1

[ 中文名 ]:
氯非铵甲苯磺酸盐

[ 英文名 ]:
Clofilium tosylate

[英文别名 ]:

Clofilium tosylate
Prestwick_682

氯非铵甲苯磺酸盐生物活性

[ 描述 ]:

Clofilium tosylate 是一种钾通道 (potassium channel) 阻滞剂,作用于人早幼粒细胞白血病 (HL-60) 细胞,激活 caspase-3 而诱导凋亡。具有抗心律失常作用。

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 心血管疾病

信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

Potassium channel[1]

[体外研究]

用Clofilium(0-20μM; 24,48和72小时)处理的HL-60细胞以时间和浓度依赖性方式导致活力和增殖的抑制。用2.5μM至10μM的Clofilium处理的HL-60细胞中细胞活力显着降低[1]。 Clofilium(10μM,12小时)诱导非活性procaspase-3,p34蛋白水解切割成其活性形式,p17,并在暴露于10mM Clofilium后2小时随后切割其底物PARP。然而,Bcl-2和Bax蛋白的表达没有显着变化[1]。细胞活力测定[1]细胞系：HL-60细胞浓度：0-20μM孵育时间：24,48和72小时结果：抑制HL-60细胞,IC50为6.3μM,24小时,3.4μM,48小时,分别为2.4μM,72小时。蛋白质印迹分析[1]细胞系：HL-60细胞浓度：10μM孵育时间：12小时结果：诱导蛋白水解切割半胱天冬酶-3并随后切割其底物PARP,而Bcl-2和Bax蛋白未改变。

[参考文献]

[1]. Choi BY, et al. Clofilium, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Cancer Lett. 1999 Dec 1;147(1-2):85-93.

氯非铵甲苯磺酸盐物理化学性质

[ 分子式 ]:
C₂₈H₄₄ClNO₃S

[ 分子量 ]:
510.172

[ 精确质量 ]:
509.273041

[ PSA ]:
65.58000

[ LogP ]:
8.46960

[ 储存条件 ]:
2-8℃

氯非铵甲苯磺酸盐MSDS

详细MSDS(安全技术说明书)

氯非铵甲苯磺酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CY9040870

CAS REGISTRY NUMBER :: 92953-10-1

LAST UPDATED :: 198910

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C21-H37-Cl-N.C7-H7-O3-S

MOLECULAR WEIGHT :: 510.24

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 :: 456 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 2,103,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 416 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 2,103,1984

氯非铵甲苯磺酸盐安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
22

[ 安全声明 (欧洲) ]:
36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
CY9040870

氯非铵甲苯磺酸盐文献

Block of heart potassium channels by clofilium and its tertiary analogs: relationship between drug structure and type of channel blocked.

Mol. Pharmacol. 34 , 60-66, (1988)

The whole-cell arrangement of the patch clamp was used to study delayed rectifier and inward rectifier K channels in isolated guinea pig ventricular cells. Block of these channels by an externally app...

The differential response of normal and ischaemic Purkinje fibres to clofilium, d-sotalol and bretylium.

Cardiovasc. Res. 23 , 554-559, (1989)

To determine whether ischaemic tissue is more sensitive than normal tissue to class III anti-arrhythmic agents, we studied the effects of the class III agents clofilium, d-sotalol and bretylium on nor...

Clofilium and other class III agents. Steinberg, et al., Williams, et al.

Handbook of Experimental Pharmacology Berlin Heidelberg 89 , 389, (1989)

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