Dequalinium ChlorideCAS号: 522-51-0分子式: C30H40N4.2Cl分子量: 527.57描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM. |
纯度 |
>98%
|
储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
|
基本信息 | |
别名 |
地喹氯铵
|
外观 |
类白色或乳白色粉末
|
可溶性/溶解性 |
DMSO : < 1 mg/mL (insoluble or slightly soluble);
Ethanol : < 1 mg/mL (insoluble); H2O : < 0.1 mg/mL (insoluble) |
生物活性 | |
靶点 |
PKC
|
In vitro(体外研究) |
Dequalinium chloride (DECA) is a cationic, lipophilic compound with structure similar to the dye rhodamine 123. DECA is selectively accumulated and retained within the mitochondria of carcinoma cells where it acts as a mitochondrial poison by blocking mitochondrial enzymes which can then disrupt cellular energy production, eventually resulting in cell death. Dequalinium Chloride is a blocker of ganglionic transmission (EC50 = 2 μM). Dequalinium is a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle. Dequalinium blocks angiotensin II-evoked K+ loss with an IC50 of 1.5 μM and also inhibited125I – monoiodoapamin binding with Ki of 1.1 μM. Dequalinium produces a rapid and reversible inhibition of the slow apamin-sensitive component of the afterhyperpolarization (AHP) which follows a single action potential in cultured rat sympathetic neurones. Dequalinium Chloride (DECA) is a dicationic lipophilic PKC inhibitor. When exposed to UV light, DECA covalently binds to and irreversibly inhibits PKCα and PKCβ.
|
In vivo(体内研究) |
In mice bearing bladder MB49 tumors, Dequalinium chloride (2 mg/kg/d, i.p.) displays anticarcinoma activity with T/C of 210%.
|
分子结构图