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Submit ReviewU 73122
Description: Phospholipase C inhibitor
Chemical Name: 1-[6-[[(17β)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
Sold with the permission of Pharmacia
Technical Data for U 73122
| M. Wt | 464.65 |
| Formula | C29H40N2O3 |
| Storage | Store at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility for U 73122
Please refer to these solubility guidelines for U 73122 (Cat. No. 1268).
Product Datasheets for U 73122
References for U 73122
References are publications that support the biological activity of the product.
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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Keywords: U 73122, U 73122 supplier, Phospholipases, C, inhibitors, inhibits, PC-PLC, PI-PLC, Esterases, U73122, Phospholipase, TRPM, 1268, Tocris Bioscience
86 Citations for U 73122
Citations are publications that use Tocris products. Selected citations for U 73122 include:
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
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
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
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
Do you know of a great paper that uses U 73122 from Tocris? Please let us know.
Reviews for U 73122
Average Rating: 5 (Based on 3 Reviews.)
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Great product..
By
Mohammad Alqudah on 10/19/2022
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Smooth muscle
Great product. Used 10 uM to inhibit ACh-induced contraction in an organ bath of smooth muscle strips.
great product.
By
Anonymous on 03/26/2020
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Hippocampal neuron
100 μM treat 45min
used this drug as an inhibitor.
By
Eric Wang on 10/05/2017
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: macrophages
Pretreat mouse macrophage cells with this inhibitor prior to the bacterial stimulation.
