U-73122是一種磷脂酶C（PLC）和5-LO（5-脂氧合酶）抑制劑，其PLC的IC50為1-2.1μM。

U-73122能有效地抑制PMN膜中受體耦聯(lián)的PLC激活[1]。U-73122能抑制人類多形核中性白細(xì)胞（PMN）的N-甲基-甲硫氨酰-亮氨酰-苯丙氨酸誘導(dǎo)的聚集以及IP3和二酰甘油的相關(guān)產(chǎn)生[2]。U-73122能顯著抑制oxotremorine-M或鳥苷酸-5'-O-（3-硫基三磷酸）誘導(dǎo)的肌醇磷酸酯釋放，而對于由加入的Ca2+誘導(dǎo)的釋放則無顯著影響[3]。

U-73122顯著減弱TNF-α mRNA的表達(dá)，對假手術(shù)動物沒有影響，但會顯著增加內(nèi)毒素血癥小鼠的心臟工作量、收縮和舒張速率，而不影響心率[4]。U-73122（400 nM/μL）顯著減少雌二醇和孕激素預(yù)處理的倉鼠的總勾欠持續(xù)時間，與VTA的車輛輸入相比。VTA輸入U-73122不會改變倉鼠在活動監(jiān)視器中的運(yùn)動行為，但是用于SKF38393的動物與用于muscimol的動物相比，伴隨有顯著的橫梁數(shù)量降低[5]。

產(chǎn)品性質(zhì)：

Cas No.:112648-68-7

別名: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

化學(xué)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

儲存條件:Store at -20°C

注意事項(xiàng)：

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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]. H?rnig 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.