CAS:112648-68-7U-73122

U-73122 is an inhibitor of phospholipase C, phospholipase A2, and 5-LO(5-lipoxygenase).

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18817579266

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18817579266

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实验数据

技术信息

CAS号

112648-68-7

储存条件

分子式

C29H40N2O3

运输

蓝冰

分子量

464.64

别名

溶解度

DMSO	33.0 mg/mL (71.0 mM)
Water	insoluble

动物实验配方

5% DMF+40% PEG300+5% Tween80+50% water

1 mg/mL

生物活性

描述U73122 is an unselective PLC inhibitor. U73122 has been utilized extensively to probe PLC signalling in cells of the immune system, in neurons and in cardiomyocytes, among many other cell types. U73122 has also been used to analyse the PI(4,5)P₂-dependence of ion channels during activation of the PLC pathway in native tissues and in heterologous expression systems. U73122 activates ion channels with yet unknown molecular identity in a variety of cell types. U73122 also reduces Ca²⁺ influx through direct actions on Ca²⁺ channels or indirectly by reducing the driving force for Ca²⁺ entry, that is, through activation of ion channels causing membrane potential depolarization. U73122 was shown to inhibit K⁺ channels and to induce the release of Ca²⁺ from intracellular stores into the cytoplasm in a PLC-independent manner.
作用机制U73122 is an N-substituted maleimide, which alkylates biological nucleophils (including cysteine residues) covalently conjugating the compound to the protein. U73122 most probably inhibits PLC through such alkylation of cysteine residues.^[1]
动物研究
剂量
Mice: 5 μl/mouse^[2] (i.c.v.); 10 ml/kg^[2] (s.c.); 9 mg/kg^[3] (i.p.), 30 mg/kg^[4] (i.p.)

给药途径
i.c.v., s.c., i.p.

动物研究
剂量	Mice: 5 μl/mouse^[2] (i.c.v.); 10 ml/kg^[2] (s.c.); 9 mg/kg^[3] (i.p.), 30 mg/kg^[4] (i.p.)
给药途径	i.c.v., s.c., i.p.