U-73122
目录号: PL06748 纯度: ≥98%
CAS No. :112648-68-7
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中文名称
U-73122
中文别名
2,4,4’-三甲基三苯胺;2,4,4'-三甲基三苯胺;U73122 抑制剂;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
英文名称
U-73122
英文别名
1H-Pyrrole-2,5-dione,1-[6-[[(17b)-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-;U 73122;U-73122;U73122(U-73122);U 73122,1-[6-[[(17β)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione;U-73122 hydrate;1-[6-[[(17beta)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione;U-73312;U-73122 hydrate(U73122);1-(6-((3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione;1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione;1-[6-[((17β)-3-methoxyestra-1,3,5[10]-trien-17-yl)amino]hexyl]-1h-pyrrole-2,5-dione;1-[6-[[(17B)-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL]AMINO]HEXYL]-1H-PYRROLE-2,5-DIONE;1-[6-((17BETA-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL)AMINO)HEXYL]-1H-PYRROLE-2,5-DIONE;U-73122 98%;U-73122 hydrate;U73122;C29H40N2O3;MolMap_000051
Cas No.
112648-68-7
分子式
C29H40N2O3
分子量
464.64
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
U-73122 是有效的 磷脂酶 C (phospholipase C) 和 5-脂氧合酶 (5-LO (5-lipoxygenase)) 抑制剂,对磷脂酶 C 的 IC50 值约为 1-2.1 µM.
生物活性
U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC 50 of 1-2.1 μM for PLC.
性状
Solid
IC50 & Target[1][2]
5-LOX
体外研究(In Vitro)
U-73122 potently inhibits receptor-coupled activation of PLC in membranes isolated from PMNs. U-73122 inhibits N-formyl-methionyl-leucyl-phenylalanine-induced aggregation of human polymorphonuclear neutrophils (PMN) and the associated production of IP3 and diacyglycerol. U-73122 markedly inhibits inositol phosphate release elicited by either oxotremorine-M or guanosine-5-O-(3-thiotriphosphate) than that induced by added Ca in digitonin-permeabilized cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (26.90 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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