氯非铵甲苯磺酸盐
| 中文名称 | 氯非铵甲苯磺酸盐 |
|---|---|
| 中文同义词 | 氯非铵甲苯磺酸盐 |
| 英文名称 | CLOFILIUM TOSYLATE |
| 英文同义词 | CLOFILIUM TOSYLATE;4-chloro-n,n-diethyl-n-heptyl-benzenebutanaminiusaltwith4-methylbenzenes;4-CHLORO-N,N-DIETHYL-N-HEPTYLBENZENEBUTANAMINIUM TOSYLATE;N-(4-(4-CHLOROPHENYL)BUTYL)-N,N-DIETHYLHEPTAN-1-AMINIUM 4-METHYLBENZENESULFONATE;Clofilium tosylate,Potassium Channel,Clofilium,inhibit,Apoptosis,Inhibitor,KcsA |
| CAS号 | 92953-10-1 |
| 分子式 | C28H44ClNO3S |
| 分子量 | 510.17 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 92953-10-1.mol |
| 结构式 |  |
氯非铵甲苯磺酸盐 性质
| 储存条件 | 4°C, protect from light |
|---|---|
| 溶解度 | 可溶于水中 |
| 形态 | 固体 |
| 颜色 | 白色 |
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。
Potassium channel
HL-60 cells treated with Clofilium (0-20 μM; 24, 48, and 72 hours) lead to suppression of viability and proliferation in both time and concentration-dependent manners. Cell viability decreases significantly in HL-60 cells treated with 2.5 μM to 10 μM of Clofilium.
Clofilium (10 μM, 12 hours) induces the proteolytic cleavage of inactive procaspase-3, p34 into its active form, p17 and subsequent cleavage of its substrate PARP at 2 h after exposure to 10 mM Clofilium. However, there is no significant change in expression of Bcl-2 and Bax proteins.
Cell Viability Assay
| Cell Line: | HL-60 cells |
| Concentration: | 0-20 μM |
| Incubation Time: | 24, 48, and 72 hours |
| Result: | Inhibited HL-60 cells with IC 50 s of 6.3 μM for 24 hours, 3.4 μM for 48 hours, 2.4 μM for 72 hours, respectively. |
Western Blot Analysis
| Cell Line: | HL-60 cells |
| Concentration: | 10 μM |
| Incubation Time: | 12 hours |
| Result: | Induced proteolytic cleavage of caspase-3 and subsequent cleavage of its substrate, PARP, while Bcl-2 and Bax proteins were unaltered. |
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