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CAS No.: 112648-68-7

U-73122 Catalog No. CSN12944

Synonyms: U-73122

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

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400-920-2911

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实验方案

技术信息

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^[2].
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.^[2]
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
human Jurkat cells - Function assay - Inhibition of human telomerase activity in human Jurkat cells by TRAP assay, IC50=0.2 μM 24053596
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.
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human Jurkat cells	-	Function assay	-	Inhibition of human telomerase activity in human Jurkat cells by TRAP assay, IC50=0.2 μM	24053596

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.

[1] Leitner MG, Michel N, et al. Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122. Br J Pharmacol. 2016 Aug;173(16):2555-69.
[2] Leitner MG, Michel N, Behrendt M, Dierich M, Dembla S, Wilke BU, Konrad M, Lindner M, Oberwinkler J, Oliver D. Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122. Br J Pharmacol. 2016 Aug;173(16):2555-69. doi: 10.1111/bph.13538. Epub 2016 Jul 18. PMID: 27328745; PMCID: PMC4959952.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1522 mL
- 10.7610 mL
- 21.5221 mL
- 5 mM
- 0.4304 mL
- 2.1522 mL
- 4.3044 mL
- 10 mM
- 0.2152 mL
- 1.0761 mL
- 2.1522 mL

技术信息

CAS号

112648-68-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H40N2O3

运输

蓝冰

分子量

464.64

别名

U-73122

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

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