U-73122

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Chemical Structure| 112648-68-7 同义名 : -
CAS号 : 112648-68-7
货号 : A877124
分子式 : C29H40N2O3
纯度 : 98%
分子量 : 464.64
MDL号 : MFCD00893825
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
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[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
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human Jurkat cells Function assay Inhibition of human telomerase activity in human Jurkat cells by TRAP assay, IC50=0.2 μM 24053596
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.52mL

4.30mL

2.15mL

参考文献

[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.