上海源葉生物科技有限公司

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聯(lián)人:
何小姐
話:
86-021-61559134
機:
15921386130
真:
86-021-55068248
址:
上海市松江區(qū)長塔路465號6幢
編:
200433
網(wǎng)址:
www.shyuanye.com
鋪:
http://true-witness.com/st191837/
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S81212
S81212
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【簡單介紹】
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  • 提示:詳情請下載說明書。
  • 產(chǎn)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.
  • 靶點: 5-LOX
  • 體內(nèi)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
  • 參考文獻:
    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. 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.
  • 溶解度: DMSO  :  12.5  mg/mL  (26.90  mM;  Need  ultrasonic)
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    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:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的性,僅供客戶參考交流研究之用。
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