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• 产品描述： U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.

• 靶点： 5-LOX

• 体内研究： U73122 significantly attenuates TNF-α mRNA expression, has no effect on sham animals, but significantly increases heart work and rate of contraction and relaxation without affecting heart rate in endotoxemic mice. U73122 (400 nM/μL) significantly reduces total lordosis durations, compared to vehicle infusions to the VTA, of oestradiol and progesterone-primed hamsters. VTA infusions of U73122 do not alter motor behaviour of hamsters in the activity monitor, but there is a significant effect of muscimol to decrease total number of beam breaks compared to hamsters administered SKF38393

• 参考文献：
  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. 7. Xie W, et al. 3Beta-hydroxy-6-aza-cholestane and related analogues as phosphatidylinositol specific phospholipase C (PI-PLC) inhibitors with antitumor activity. Bioorg Med Chem. 2000 Apr;8(4):699-706.

• 溶解性： DMSO  :  12.5  mg/mL  (26.90  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.152 ml	10.761 ml	21.522 ml
  5 mM	0.43 ml	2.152 ml	4.304 ml
  10 mM	0.215 ml	1.076 ml	2.152 ml
  50 mM	0.043 ml	0.215 ml	0.43 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *