U-73122是一种磷脂酶C（PLC）和5-LO（5-脂氧合酶）抑制剂，其PLC的IC50为1-2.1µM。

U-73122能有效地抑制PMN膜中受体耦联的PLC激活[1]。U-73122能抑制人类多形核中性白细胞（PMN）的N-甲基-甲硫氨酰-亮氨酰-苯丙氨酸诱导的聚集以及IP3和二酰甘油的相关产生[2]。U-73122能显著抑制oxotremorine-M或鸟苷酸-5'-O-（3-硫基三磷酸）诱导的肌醇磷酸酯释放，而对于由加入的Ca2+诱导的释放则无显著影响[3]。

U-73122显著减弱TNF-α mRNA的表达，对假手术动物没有影响，但会显著增加内毒素血症小鼠的心脏工作量、收缩和舒张速率，而不影响心率[4]。U-73122（400 nM/μL）显著减少雌二醇和孕激素预处理的仓鼠的总勾欠持续时间，与VTA的车辆输入相比。VTA输入U-73122不会改变仓鼠在活动监视器中的运动行为，但是用于SKF38393的动物与用于muscimol的动物相比，伴随有显著的横梁数量降低[5]。

产品性质：

Cas No.:112648-68-7

别名:1-[6-[((17Β)-3-雌酮-1,3,5[10]-三烯-17-基)氨基]乙基]-1H-吡咯-2,5-二酮

化学名: 1-[6-[[(8R,9S,13S,14S,17S)-3-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl]amino]hexyl]pyrrole-2,5-dione

Canonical SMILES:CC12CCC3C(C1CCC2NCCCCCCN4C(=O)C=CC4=O)CCC5=C3C=CC(=C5)OC

分子式:C29H40N2O3

分子量:464.64

溶解度:≥ 5.67mg/mL in DMSO with gentle warming, ≥ 15.5mg/mL in EtOH with ultrasonic and warming

储存条件:Store at -20°C

注意事项：

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References:

[1]. Smith RJ, et al. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. J Pharmacol Exp Ther. 1990 May;253(2):688-97.

[2]. Bleasdale JE, et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther. 1990 Nov;255(2):756-68.

[3]. Thompson AK, et al. The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation. J Biol Chem. 1991 Dec 15;266(35):23856-62.

[4]. Peng T, et al. Disruption of phospholipase Cgamma1 signalling attenuates cardiac tumor necrosis factor-alpha expression and improves myocardial function during endotoxemia. Cardiovasc Res. 2008 Apr 1;78(1):90-7. Epub 2007 Dec 12.

[5]. Frye CA, et al. In the ventral tegmental area, the membrane-mediated actions of progestins for lordosis of hormone-primed hamsters involve phospholipase C and protein kinase C. J Neuroendocrinol. 2007 Sep;19(9):717-24.

[6]. Hörnig M, et al. Inhibition of 5-lipoxygenase by U73122 is due to covalent binding to cysteine 416. Biochim Biophys Acta. 2012 Feb;1821(2):279-86.