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U 73122

Cat. No. 1268 86 篇引用文献 3 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Phospholipase C inhibitor
化学名： 1-[6-[[(17β)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione
纯度： ≥98% (HPLC)
说明书
引用文献 (86)
评论 (3)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for U 73122

U 73122 is a phospholipase C inhibitor. Inhibits agonist-induced platelet aggregation with IC50 values of 1-5 μM. Potently inhibits human polymorphonuclear neutrophil adhesion on biological surfaces (IC50 < 50 nM) and exhibits antinociceptive activity in vivo. Also activates TRPM4 and inhibits TRPM3 channels.

Negative Control also available.

许可信息

Sold with the permission of Pharmacia

技术数据 for U 73122

分子量 464.65
公式 C29H40N2O3
储存 Store at RT
纯度 ≥98% (HPLC)
CAS Number 112648-68-7
PubChem ID 104794
InChI Key LUFAORPFSVMJIW-ZRJUGLEFSA-N
Smiles [H][C@]23[C@@]([C@]([H])(CC[C@@H]4NCCCCCCN5C(C=CC5=O)=O)[C@]4(C)CC3)([H])CCC1=CC(OC)=CC=C12

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性 for U 73122

请参阅 U 73122（目录编号 1268）溶解性指南。

产品说明书 for U 73122

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for U 73122

参考文献是支持产品生物活性的出版物。

Bleasdale et al (1990) Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J.Pharmacol.Exp.Ther. 255 756 PMID: 2147038

Shi et al (2008) Phospholipase Cβ3 in mouse and human dorsal root ganglia and spinal cord is a possible target for treatment of neuropathic pain. Proc.Natl.Acad.Sci.U.S.A. 105 20004 PMID: 19066214

Smith et al (1996) U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions. J.Pharmacol.Exp.Ther. 278 320 PMID: 8764366

Leitner et al (2016) Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122. Br.J.Pharmacol. 173 2555 PMID: 27328745

If you know of a relevant reference for U 73122, please let us know.

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关键词: U 73122, U 73122 supplier, Phospholipases, C, inhibitors, inhibits, PC-PLC, PI-PLC, Esterases, U73122, Phospholipase, TRPM, 1268, Tocris Bioscience

86 篇 U 73122 的引用文献

引用文献是使用了 Tocris 产品的出版物。 U 73122 的部分引用包括：

Franchini et al (2019) Linking NMDA Receptor Synaptic Retention to Synaptic Plasticity and Cognition. iScience 19 927 PMID: 31518901

Pitt et al (2017) Neuroprotective astrocyte-derived Ins./IGF-1 stimulates endocytic processing and extracellular release of neuron-bound Aβ oligomers. Mol Biol Cell 28 2623 PMID: 28963439

Berrout et al (2017) TRPA1-FGFR2 binding event is a regulatory oncogenic driver modulated by miRNA-142-3p. Nat Commun 8 947 PMID: 29038531

Qu et al (2016) Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine. World J Gastrointest Pathophysiol 7 150 PMID: 26909238

Townsend and Emala (2013) Quercetin acutely relaxes airway smooth muscle and potentiates β-agonist-induced relaxation via dual phosphodiesterase inhibition of PLCβ and PDE4. Am J Physiol Lung Cell Mol Physiol 305 L396 PMID: 23873842

López-Sanjurjo et al (2013) Lysosomes shape Ins(1,4,5)P3-evoked Ca2+ signals by selectively sequestering Ca2+ released from the endoplasmic reticulum. J Cell Sci 126 289 PMID: 23097044

Caiati et al (2013) PrPC controls via protein kinase A the direction of synaptic plasticity in the immature hippocampus. J Neurosci 33 2973 PMID: 23407955

Melchior and Frangos (2012) Gαq/11-mediated intracellular calcium responses to retrograde flow in endothelial cells. J Pharmacol Exp Ther 303 C467 PMID: 22700794

Zhao et al (2010) Melatonin potentiates glycine currents through a PLC/PKC signalling pathway in rat retinal ganglion cells. J Physiol 588 2605 PMID: 20519319

Huang and Hsu (2010) Activation of muscarinic acetylcholine receptors induces a nitric oxide-dependent long-term depression in rat medial prefrontal cortex. Cereb Cortex 20 982 PMID: 19666830

Olianas et al (2016) The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors European Journal of Pharmacology 794 135 PMID: 27876620

Guemez-Gamboa et al (2014) Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching. Neuron 82 1004 PMID: 24908484

Zhao (2014) BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling. J Neurophysiol 111 1008 PMID: 24335212

Rojas et al (2013) Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors. Mol Pharmacol 83 106 PMID: 23066089

Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333

Jiang et al (2010) The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period. Neuron 66 248 PMID: 20435001

Cvetkovic-Lopes et al (2010) Rat hypocretin/orexin neurons are maintained in a depolarized state by TRPC channels. PLoS One 5 e15673 PMID: 21179559

Sowa et al (2010) Prostatic acid phosphatase reduces thermal sensitivity and chronic pain sensitization by depleting phosphatidylinositol 4,5-bisphosphate. J Neurosci 30 10282 PMID: 20685973

Eno et al (2018) Slow calcium waves mediate furrow microtubule reorganization and germ plasm compaction in the early zebrafish embryo. Development 145 PMID: 29632136

Lin et al (2018) The Allergen Der p3 from House Dust Mite Stimulates Store-Operated Ca2+ Channels and Mast Cell Migration through PAR4 Receptors. Mol Cell 70 228 PMID: 29677491

Wang et al (2016) The prostaglandin E2-EP3 receptor axis regulates Anaplasma phagocytophilum-mediated NLRC4 inflammasome activation. PLoS Pathog. 12 e1005803 PMID: 27482714

Sato et al (2015) Intercellular Odontoblast Communication via ATP Mediated by Pannexin-1 Channel and Phospholipase C-coupled Receptor Activation. PLoS One 6 326 PMID: 26617529

Rioult-Pedotti et al (2015) DA Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation. PLoS One 10 e0124986 PMID: 25938462

Szteyn et al (2015) Divergence in endothelin-1- and bradykinin-activated store-operated calcium entry in afferent sensory neurons. PLoS One 7 PMID: 25873305

Liu et al (2015) A long-acting β2-adrenergic agonist increases the expression of muscarine cholinergic subtype-3 receptors by activating the β2-adrenoceptor cyclic adenosine monophosphate signaling pathway in airway smooth muscle cells. Sci Rep 11 4121 PMID: 25672589

Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Mediators Inflamm 5 10468 PMID: 26020477

Yoon et al (2015) The Effect of Therapeutic Blockades of Dust Particles-Induced Ca2+ Signaling and Proinflammatory Cytokine IL-8 in Human Bronchial Epithelial Cells. Blood 2015 843024 PMID: 26640326

Magwenzi et al (2015) Oxidized LDL activates blood platelets through CD36/NOX2-mediated inhibition of the cGMP/protein kinase G signaling cascade. PLoS One 125 2693 PMID: 25710879

Manosalva et al (2015) Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils. Sci Rep 10 e0119715 PMID: 25790461

Ang et al (2015) The short-chain fatty acid receptor GPR43 is transcriptionally regulated by XBP1 in human monocytes. MBio 5 8134 PMID: 25633224

Azab et al (2015) Binding of αherpesvirus Glycoprotein H to Surface α4β1-Integrins Activates Calcium-Signaling Pathways and Induces Phosphatidylserine Exposure on the Plasma Membrane. Sci Rep 6 PMID: 26489864

Pandya and Pillai (2014) TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis. J Neurophysiol 12 47 PMID: 25052836

Bailes et al (2012) Reproducible and sustained regulation of Gαs signalling using a metazoan opsin as an optogenetic tool. Neuron 7 e30774 PMID: 22292038

Garrett et al (2012) γ-protocadherins control cortical dendrite arborization by regulating the activity of a FAK/PKC/MARCKS signaling pathway. Proc Natl Acad Sci U S A 74 269 PMID: 22542181

Huang et al (2012) SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes. Oncotarget 7 e49954 PMID: 23185493

Xiao et al (2018) OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons. Elife 7 PMID: 29676731

Bushart et al (2018) Targeting potassium channels to treat cerebellar ataxia. Ann Clin Transl Neurol 5 297 PMID: 29560375

Hellmer et al (2018) A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina. Physiol Rep 6 e13885 PMID: 30338673

Lim et al (2018) Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures. Int J Mol Sci 19 PMID: 30274399

Atakpa et al (2018) IP3 Receptors Preferentially Associate with ER-Lysosome Contact Sites and Selectively Deliver Ca2+ to Lysosomes. Cell Rep 25 3180 PMID: 30540949

Osman et al (2016) Detachment of surface membrane invagination systems by cationic amphiphilic drugs. ASN Neuro 6 18536 PMID: 26725955

Lau et al (2011) Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium. Carcinogenesis 300 C113 PMID: 21068362

Dai et al (2011) Phospholipase C, Ca2+, and calmodulin signaling are required for 5-HT2A receptor-mediated transamidation of Rac1 by transglutaminase. J Biol Chem 213 403 PMID: 20717650

Babola et al (2020) Purinergic signaling in cochlear supporting cells reduces hair cell excitability by increasing the extracellular space. ELife 9 e52160 PMID: 31913121

Pleil et al (2015) NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking. Nat Neurosci 18 545 PMID: 25751534

Amitani et al (2015) Allantoin ameliorates chemically-induced pancreatic β-cell damage through activation of the imidazoline I3 receptors. PeerJ 3 e1105 PMID: 26290782

Tabatadze et al (2015) Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus. J Neurosci 35 11252 PMID: 26269634

Mitrugno et al (2014) A novel and essential role for FcγRIIa in cancer cell-induced platelet activation. Blood 123 249 PMID: 24258815

Boyd-Tressler et al (2014) Chemotherapeutic drugs induce ATP release via caspase-gated pannexin-1 channels and a caspase/pannexin-1-independent mechanism. J Biol Chem 289 27246 PMID: 25112874

Morelli et al (2014) Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation. BMC Cancer 14 921 PMID: 25481381

Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316 PMID: 25181481

Tsai et al (2014) A polarized Ca2+, diacylglycerol and STIM1 signalling system regulates directed cell migration. Nat Cell Biol 16 133 PMID: 24463606

Tang et al (2014) Lactate-mediated glia-neuronal signalling in the mammalian brain. Nat Commun 5 3284 PMID: 24518663

Aihara et al (2013) In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium. Proc Natl Acad Sci U S A 288 33585 PMID: 24121509

Chang et al (2013) Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition. Psychopharmacology (Berl) 34 1096 PMID: 23349021

Shi et al (2008) Phospholipase C{β}3 in mouse and human dorsal root ganglia and spinal cord is a possible target for treatment of neuropathic pain. Front Physiol 105 20004 PMID: 19066214

Shi (2017) The novel cannabinoid receptor GPR55 mediates anxiolytic-like effects in the medial orbital cortex of mice with acute stress. Mol Brain 10 38 PMID: 28800762

Kishore and Hall (2017) Disease-associated extracellular loop mutations in the adhesion G protein-coupled receptor G1 (ADGRG1; GPR56) differentially regulate downstream signaling. J Biol Chem 292 9711 PMID: 28424266

Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882

Rajan et al (2017) A Mechanism Coupling Systemic Energy Sensing to Adipokine Secretion. Dev Cell 43 83 PMID: 29017032

Glovaci and Chapman (2015) Activation of Phosphatidylinositol-Linked DA Receptors Induces a Facilitation of Glutamate-Mediated Synaptic Transmission in the Lateral Entorhinal Cortex. PLoS One 10 e0131948 PMID: 26133167

Mariqueo et al (2014) Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons. Mol Med Rep 111 1940 PMID: 24572089

Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. Oncotarget 5 3145 PMID: 24762669

Korb et al (2013) Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity. Nat Neurosci 16 874 PMID: 23749147

Pal et al (2013) Divergent β-arrestin-dependent signaling events are dependent upon sequences within G-protein-coupled receptor C termini. J Biol Chem 288 3265 PMID: 23235155

Grassin-Delyle et al (2013) The expression and relaxant effect of bitter taste receptors in human bronchi. Respir Res 14 134 PMID: 24266887

Valero et al (2011) Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin 32 487 PMID: 21441943

Okada et al (2011) High extracellular Ca2+ stimulates Ca2+-activated Cl- currents in frog parathyroid cells through the mediation of arachidonic acid cascade. PLoS One 6 e19158 PMID: 21559478

Moore et al (2009) Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors. Neuron 61 287 PMID: 19186170

Roebber et al (2019) The Role of the Anion in Salt (NaCl) Detection by Mouse Taste Buds. J Neurosci 39 6224 PMID: 31171579

Kim et al (2019) Role of miRNA-181a-2-3p in cadmium-induced inflammatory responses of human bronchial epithelial cells. J Thorac Dis 11 3055 PMID: 31463135

Bigford et al (2012) 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization. J Biol Chem 287 11049 PMID: 22291020

Hurt (2012) PAPupuncture has localized and long-lasting antinociceptive effects in mouse models of acute and chronic pain. Mol Pain 8 28 PMID: 22524543

Song et al (2009) Signal transduction mechanisms underlying group I mGluR-mediated increase in frequency and amplitude of spontaneous EPSCs in the spinal trigeminal subnucleus oralis of the rat. Mol Pain 5 50 PMID: 19725970

Bagayogo and Dreyfus (2009) Regulated release of BDNF by cortical oligodendrocytes is mediated through metabotropic glutamate receptors and the PLC pathway. ASN Neuro 1 PMID: 19570026

Dai et al (2008) A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients. Neurosignals 16 112 PMID: 18253052

Liu et al (2007) Angiotensin II inhibits native bTREK-1 K+ channels through a PLC-, kinase C-, and PIP2-independent pathway requiring ATP hydrolysis. Am J Physiol Cell Physiol 293 C682 PMID: 17494631

Newman et al (2007) Endocannabinoids mediate muscarine-induced synaptic depression at the vertebrate neuromuscular junction. Eur J Neurosci 25 1619 PMID: 17408433

Yin et al (2008) Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling. Neuropharmacology 54 79 PMID: 17675102

Graham et al (2008) Melanopsin ganglion cells use a membrane-associated rhabdomeric phototransduction cascade. J Neurophysiol 99 2522 PMID: 18305089

Johnston et al (2008) Cholinergic-induced Ca2+ signaling in interstitial cells of Cajal from the guinea pig bladder. Am J Physiol Renal Physiol 294 F645 PMID: 18171995

Krjukova et al (2004) Phospholipase C activator m-3M3FBS affects Ca2+ homeostasis independently of phospholipase C activation. Br J Pharmacol 143 3 PMID: 15302681

Pierre et al (2004) PAM mediates sustained inhibition of cAMP signaling by sphingosine-1-phosphate. EMBO J 23 3031 PMID: 15257286

Fresco et al (2004) Facilitation of noradrenaline release by activation of adenosine A(2A) receptors triggers both phospholipase C and adenylate cyclase pathways in rat tail artery. Cardiovasc Res 63 739 PMID: 15306230

Nishi et al (2003) Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. Am J Physiol Cell Physiol 100 1322 PMID: 12538871

Jackson et al (2005) Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction. Am J Physiol Cell Physiol 314 1109 PMID: 15901799

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Great product..
By Mohammad Alqudah on 10/19/2022
分析类型： In Vitro
种属： Rat
细胞系/组织： Smooth muscle

Great product. Used 10 uM to inhibit ACh-induced contraction in an organ bath of smooth muscle strips.

review image
great product.
By Anonymous on 03/26/2020
分析类型： In Vitro
种属： Rat
细胞系/组织： Hippocampal neuron

100 μM treat 45min

review image
used this drug as an inhibitor.
By Eric Wang on 10/05/2017
分析类型： In Vitro
种属： Mouse
细胞系/组织： macrophages

Pretreat mouse macrophage cells with this inhibitor prior to the bacterial stimulation.

PMID: 27482714
review image