Dequalinium Chloride,522-51-0

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产品名称：Dequalinium Chloride

产品别名：地喹氯铵

英文别名：Dequalinium Chloride

靶点：PKC

CAS：522-51-0

纯度：>98%

外观：类白色或乳白色粉末

保存方法：-20°C 冷藏长期储存,常温运输及临时存放

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.

溶解性：易溶于沸水，遇光易变质。

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.

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%.

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