Dequalinium Chloride

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

Dequalinium Chloride