Home / Phospholipase Inhibitors / U 73122

U 73122

Catalog #: 1268
86 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1268/10
1268/50
U 73122 | CAS No. 112648-68-7 | Phospholipase Inhibitors
1 Image
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%

Product Details
Citations (86)
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Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:
464.65
Formula:
C29H40N2O3
Solubility:
Solubility guidelines for U 73122
Purity:
≥98%
Storage:
Store at RT
CAS No:
112648-68-7

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.

Additional Information

Licensing Caveats:
Sold with the permission of Pharmacia
Other Product-Specific Information:

Background References

  1. Connexin 43 hemichannels contribute to cytoplasmic Ca2+ oscillations by providing a bimodal Ca2+-dependent Ca2+ entry pathway.
    De Bock M, Wang N, Bol M, Decrock E, Ponsaerts R, Bultynck G, Dupont G, Leybaert L
    J. Biol. Chem., 2012;287(15):12250-66.
  2. Platelet Ca(2+) responses coupled to glycoprotein VI and Toll-like receptors persist in the presence of endothelial-derived inhibitors: roles for secondary activation of P2X1 receptors and release from intracellular Ca(2+) stores.
    Fung CY, Jones S, Ntrakwah A, Naseem KM, Farndale RW, Mahaut-Smith MP
    Blood, 2012;119(15):3613-21.
  3. A novel and essential role for FcgammaRIIa in cancer cell-induced platelet activation.
    Mitrugno A, Williams D, Kerrigan S, Moran N
    Blood, 2013;123(2):249-60.
  4. Role of focal adhesion tyrosine kinases in GPVI-dependent platelet activation and reactive oxygen species formation.
    Carrim N, Walsh T, Consonni A, Torti M, Berndt M, Metharom P
    PLoS ONE, 2014;9(11):e113679.
  5. In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.
    Aihara, Eitaro, Hentz, Courtney, Korman, Abraham, Perry, Nicholas, Prasad, Vikram, Shull, Gary E, Montrose, Marshall
    J Biol Chem, 2013;288(47):33585-97.
  6. BNGR-A25L and -A27 are two functional G protein-coupled receptors for CAPA periviscerokinin neuropeptides in the silkworm, Bombyx mori
    Z Shen, Y Chen, L Hong, Z Cui, H Yang, X He, Y Shi, L Shi, F Han, N Zhou
    J. Biol. Chem., 2017;0(0):.
  7. SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes.
    Huang C, Wu J, Liao R, Zhang W
    PLoS ONE, 2012;7(11):e49954.
  8. Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
    Morelli, Maria Be, Amantini, Consuelo, Nabissi, Massimo, Liberati, Sonia, Cardinali, Claudio, Farfariello, Valerio, Tomassoni, Daniele, Quaglia, Wilma, Piergentili, Alessand, Bonifazi, Alessand, Del Bello, Fabio, Santoni, Matteo, Mammana, Gabriele, Servi, Lucilla, Filosa, Alessand, Gismondi, Angela, Santoni, Giorgio
    BMC Cancer, 2014;14(0):921.
  9. The Complement System Component C5a Produces Thermal Hyperalgesia via Macrophage-to-Nociceptor Signaling That Requires NGF and TRPV1

    J Neurosci, 2016;36(18):5055-70.
  10. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach-Mansky R, Sacks D, Germain R, Kastner D, Chae J
    Nature, 2012;492(7427):123-7.
  11. Specific activation of the G protein-coupled receptor BNGR-A21 by the neuropeptide corazonin from the silkworm, Bombyx mori, dually couples to the G(q) and G(s) signaling cascades.
    Yang, Jingwen, Huang, Haishan, Yang, Huipeng, He, Xiaobai, Jiang, Xue, Shi, Ying, Alatangaole, Damirin, Shi, Liangen, Zhou, Naiming
    J Biol Chem, 2013;288(17):11662-75.
  12. IP3 Receptors Preferentially Associate with ER-Lysosome Contact Sites and Selectively Deliver Ca2+ to Lysosomes
    P Atakpa, NB Thillaiapp, S Mataragka, DL Prole, CW Taylor
    Cell Rep, 2018;25(11):3180-3193.e7.
  13. RhoG protein regulates platelet granule secretion and thrombus formation in mice.
    Goggs R, Harper M, Pope R, Savage J, Williams C, Mundell S, Heesom K, Bass M, Mellor H, Poole A
    J Biol Chem, 2013;288(47):34217-29.
  14. Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122.
    Leitner et al.
    Br.J.Pharmacol., 2016;173:2555
  15. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils.
    Bleasdale et al.
    J.Pharmacol.Exp.Ther., 1990;255:756
  16. Phospholipase Cβ3 in mouse and human dorsal root ganglia and spinal cord is a possible target for treatment of neuropathic pain.
    Shi et al.
    Proc.Natl.Acad.Sci.U.S.A., 2008;105:20004
  17. U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions.
    Smith et al.
    J.Pharmacol.Exp.Ther., 1996;278:320

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Citations for U 73122

The citations listed below are publications that use Tocris products. Selected citations for U 73122 include:

86 Citations: Showing 1 - 10

  1. Purinergic signaling in cochlear supporting cells reduces hair cell excitability by increasing the extracellular space.
    Authors: Babola Et al.
    ELife  2020;9:e52160
  2. The Role of the Anion in Salt (NaCl) Detection by Mouse Taste Buds.
    Authors: Roebber Et al.
    J Neurosci  2019;39:6224
  3. Linking NMDA Receptor Synaptic Retention to Synaptic Plasticity and Cognition.
    Authors: Franchini Et al.
    iScience  2019;19:927
  4. Role of miRNA-181a-2-3p in cadmium-induced inflammatory responses of human bronchial epithelial cells.
    Authors: Kim Et al.
    J Thorac Dis  2019;11:3055
  5. The Allergen Der p3 from House Dust Mite Stimulates Store-Operated Ca2+ Channels and Mast Cell Migration through PAR4 Receptors.
    Authors: Lin Et al.
    Mol Cell  2018;70:228
  6. OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons.
    Authors: Xiao Et al.
    Elife  2018;7
  7. A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina.
    Authors: Hellmer Et al.
    Physiol Rep  2018;6:e13885
  8. Targeting potassium channels to treat cerebellar ataxia.
    Authors: Bushart Et al.
    Ann Clin Transl Neurol  2018;5:297
  9. IP3 Receptors Preferentially Associate with ER-Lysosome Contact Sites and Selectively Deliver Ca2+ to Lysosomes.
    Authors: Atakpa Et al.
    Cell Rep  2018;25:3180
  10. Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures.
    Authors: Lim Et al.
    Int J Mol Sci  2018;19
  11. Slow calcium waves mediate furrow microtubule reorganization and germ plasm compaction in the early zebrafish embryo.
    Authors: Eno Et al.
    Development  2018;145
  12. TRPA1-FGFR2 binding event is a regulatory oncogenic driver modulated by miRNA-142-3p.
    Authors: Berrout Et al.
    Nat Commun  2017;8:947
  13. A Mechanism Coupling Systemic Energy Sensing to Adipokine Secretion.
    Authors: Rajan Et al.
    Dev Cell  2017;43:83
  14. Disease-associated extracellular loop mutations in the adhesion G protein-coupled receptor G1 (ADGRG1; GPR56) differentially regulate downstream signaling.
    Authors: Kishore and Hall
    J Biol Chem  2017;292:9711
  15. Neuroprotective astrocyte-derived Ins./IGF-1 stimulates endocytic processing and extracellular release of neuron-bound Aβ oligomers.
    Authors: Pitt Et al.
    Mol Biol Cell  2017;28:2623
  16. Protein kinase D at the Golgi controls NLRP3 inflammasome activation.
    Authors: Zhang Et al.
    J Exp Med  2017;214:2671
  17. The novel cannabinoid receptor GPR55 mediates anxiolytic-like effects in the medial orbital cortex of mice with acute stress.
    Authors: Shi
    Mol Brain  2017;10(1):38
  18. Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.
    Authors: Qu Et al.
    World J Gastrointest Pathophysiol  2016;7:150
  19. The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors
    Authors: Olianas Et al.
    European Journal of Pharmacology  2016;794:135
  20. Detachment of surface membrane invagination systems by cationic amphiphilic drugs.
    Authors: Osman Et al.
    ASN Neuro  2016;6:18536
  21. The prostaglandin E2-EP3 receptor axis regulates Anaplasma phagocytophilum-mediated NLRC4 inflammasome activation.
    Authors: Wang Et al.
    PLoS Pathog.  2016;12:e1005803
  22. Divergence in endothelin-1- and bradykinin-activated store-operated calcium entry in afferent sensory neurons.
    Authors: Szteyn Et al.
    PLoS One  2015;7
  23. Intercellular Odontoblast Communication via ATP Mediated by Pannexin-1 Channel and Phospholipase C-coupled Receptor Activation.
    Authors: Sato Et al.
    PLoS One  2015;6:326
  24. Binding of αherpesvirus Glycoprotein H to Surface α4β1-Integrins Activates Calcium-Signaling Pathways and Induces Phosphatidylserine Exposure on the Plasma Membrane.
    Authors: Azab Et al.
    Sci Rep  2015;6
  25. The short-chain fatty acid receptor GPR43 is transcriptionally regulated by XBP1 in human monocytes.
    Authors: Ang Et al.
    MBio  2015;5:8134
  26. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Mediators Inflamm  2015;5:10468
  27. Allantoin ameliorates chemically-induced pancreatic β-cell damage through activation of the imidazoline I3 receptors.
    Authors: Amitani Et al.
    PeerJ  2015;3:e1105
  28. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci  2015;35:11252
  29. The Effect of Therapeutic Blockades of Dust Particles-Induced Ca2+ Signaling and Proinflammatory Cytokine IL-8 in Human Bronchial Epithelial Cells.
    Authors: Yoon Et al.
    Blood  2015;2015:843024
  30. NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking.
    Authors: Pleil Et al.
    Nat Neurosci  2015;18:545
  31. Oxidized LDL activates blood platelets through CD36/NOX2-mediated inhibition of the cGMP/protein kinase G signaling cascade.
    Authors: Magwenzi Et al.
    PLoS One  2015;125:2693
  32. 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.
    Authors: Liu Et al.
    Sci Rep  2015;11:4121
  33. Activation of Phosphatidylinositol-Linked DA Receptors Induces a Facilitation of Glutamate-Mediated Synaptic Transmission in the Lateral Entorhinal Cortex.
    Authors: Glovaci and Chapman
    PLoS One  2015;10:e0131948
  34. DA Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation.
    Authors: Rioult-Pedotti Et al.
    PLoS One  2015;10:e0124986
  35. Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils.
    Authors: Manosalva Et al.
    Sci Rep  2015;10:e0119715
  36. mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
    Authors: Kubota Et al.
    PLoS One  2014;9:e106316
  37. Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching.
    Authors: Guemez-Gamboa Et al.
    Neuron  2014;82:1004
  38. Lactate-mediated glia-neuronal signalling in the mammalian brain.
    Authors: Tang Et al.
    Nat Commun  2014;5:3284
  39. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
    Authors: Al-Ejeh Et al.
    Oncotarget  2014;5:3145
  40. Chemotherapeutic drugs induce ATP release via caspase-gated pannexin-1 channels and a caspase/pannexin-1-independent mechanism.
    Authors: Boyd-Tressler Et al.
    J Biol Chem  2014;289:27246
  41. A polarized Ca2+, diacylglycerol and STIM1 signalling system regulates directed cell migration.
    Authors: Tsai Et al.
    Nat Cell Biol  2014;16:133
  42. Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
    Authors: Morelli Et al.
    BMC Cancer  2014;14:921
  43. TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis.
    Authors: Pandya and Pillai
    J Neurophysiol  2014;12:47
  44. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood  2014;123:249
  45. Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons.
    Authors: Mariqueo Et al.
    Mol Med Rep  2014;111:1940
  46. BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling.
    Authors: Zhao
    J Neurophysiol  2014;111:1008
  47. Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors.
    Authors: Rojas Et al.
    Mol Pharmacol  2013;83:106
  48. Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition.
    Authors: Chang Et al.
    Psychopharmacology (Berl)  2013;34:1096
  49. PrPC controls via protein kinase A the direction of synaptic plasticity in the immature hippocampus.
    Authors: Caiati Et al.
    J Neurosci  2013;33:2973
  50. Quercetin acutely relaxes airway smooth muscle and potentiates β-agonist-induced relaxation via dual phosphodiesterase inhibition of PLCβ and PDE4.
    Authors: Townsend and Emala
    Am J Physiol Lung Cell Mol Physiol  2013;305:L396
  51. In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.
    Authors: Aihara Et al.
    Proc Natl Acad Sci U S A  2013;288:33585
  52. Divergent β-arrestin-dependent signaling events are dependent upon sequences within G-protein-coupled receptor C termini.
    Authors: Pal Et al.
    J Biol Chem  2013;288:3265
  53. Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity.
    Authors: Korb Et al.
    Nat Neurosci  2013;16:874
  54. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res  2013;14:134
  55. Lysosomes shape Ins(1,4,5)P3-evoked Ca2+ signals by selectively sequestering Ca2+ released from the endoplasmic reticulum.
    Authors: L&oacute;pez-Sanjurjo Et al.
    J Cell Sci  2013;126:289
  56. PAPupuncture has localized and long-lasting antinociceptive effects in mouse models of acute and chronic pain.
    Authors: Hurt
    Mol Pain  2012;8:28
  57. SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes.
    Authors: Huang Et al.
    Oncotarget  2012;7:e49954
  58. Reproducible and sustained regulation of Gαs signalling using a metazoan opsin as an optogenetic tool.
    Authors: Bailes Et al.
    Neuron  2012;7:e30774
  59. γ-protocadherins control cortical dendrite arborization by regulating the activity of a FAK/PKC/MARCKS signaling pathway.
    Authors: Garrett Et al.
    Proc Natl Acad Sci U S A  2012;74:269
  60. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Authors: Lee Et al.
    Nature  2012;492:123
  61. Gαq/11-mediated intracellular calcium responses to retrograde flow in endothelial cells.
    Authors: Melchior and Frangos
    J Pharmacol Exp Ther  2012;303:C467
  62. 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization.
    Authors: Bigford Et al.
    J Biol Chem  2012;287:11049
  63. High extracellular Ca2+ stimulates Ca2+-activated Cl- currents in frog parathyroid cells through the mediation of arachidonic acid cascade.
    Authors: Okada Et al.
    PLoS One  2011;6:e19158
  64. Contractile effect of tachykinins on rabbit small intestine.
    Authors: Valero Et al.
    Acta Pharmacol Sin  2011;32:487
  65. Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium.
    Authors: Lau Et al.
    Carcinogenesis  2011;300:C113
  66. Phospholipase C, Ca2+, and calmodulin signaling are required for 5-HT2A receptor-mediated transamidation of Rac1 by transglutaminase.
    Authors: Dai Et al.
    J Biol Chem  2011;213:403
  67. The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period.
    Authors: Jiang Et al.
    Neuron  2010;66:248
  68. Rat hypocretin/orexin neurons are maintained in a depolarized state by TRPC channels.
    Authors: Cvetkovic-Lopes Et al.
    PLoS One  2010;5:e15673
  69. Melatonin potentiates glycine currents through a PLC/PKC signalling pathway in rat retinal ganglion cells.
    Authors: Zhao Et al.
    J Physiol  2010;588:2605
  70. Prostatic acid phosphatase reduces thermal sensitivity and chronic pain sensitization by depleting phosphatidylinositol 4,5-bisphosphate.
    Authors: Sowa Et al.
    J Neurosci  2010;30:10282
  71. Activation of muscarinic acetylcholine receptors induces a nitric oxide-dependent long-term depression in rat medial prefrontal cortex.
    Authors: Huang and Hsu
    Cereb Cortex  2010;20:982
  72. Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors.
    Authors: Moore Et al.
    Neuron  2009;61:287
  73. 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.
    Authors: Song Et al.
    Mol Pain  2009;5:50
  74. Regulated release of BDNF by cortical oligodendrocytes is mediated through metabotropic glutamate receptors and the PLC pathway.
    Authors: Bagayogo and Dreyfus
    ASN Neuro  2009;1
  75. Melanopsin ganglion cells use a membrane-associated rhabdomeric phototransduction cascade.
    Authors: Graham Et al.
    J Neurophysiol  2008;99:2522
  76. Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling.
    Authors: Yin Et al.
    Neuropharmacology  2008;54:79
  77. Cholinergic-induced Ca2+ signaling in interstitial cells of Cajal from the guinea pig bladder.
    Authors: Johnston Et al.
    Am J Physiol Renal Physiol  2008;294:F645
  78. A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients.
    Authors: Dai Et al.
    Neurosignals  2008;16:112
  79. Phospholipase C{β}3 in mouse and human dorsal root ganglia and spinal cord is a possible target for treatment of neuropathic pain.
    Authors: Shi Et al.
    Front Physiol  2008;105:20004
  80. Angiotensin II inhibits native bTREK-1 K+ channels through a PLC-, kinase C-, and PIP2-independent pathway requiring ATP hydrolysis.
    Authors: Liu Et al.
    Am J Physiol Cell Physiol  2007;293:C682
  81. Endocannabinoids mediate muscarine-induced synaptic depression at the vertebrate neuromuscular junction.
    Authors: Newman Et al.
    Eur J Neurosci  2007;25:1619
  82. Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.
    Authors: Jackson Et al.
    Am J Physiol Cell Physiol  2005;314:1109
  83. Facilitation of noradrenaline release by activation of adenosine A(2A) receptors triggers both phospholipase C and adenylate cyclase pathways in rat tail artery.
    Authors: Fresco Et al.
    Cardiovasc Res  2004;63:739
  84. PAM mediates sustained inhibition of cAMP signaling by sphingosine-1-phosphate.
    Authors: Pierre Et al.
    EMBO J  2004;23:3031
  85. Phospholipase C activator m-3M3FBS affects Ca2+ homeostasis independently of phospholipase C activation.
    Authors: Krjukova Et al.
    Br J Pharmacol  2004;143:3
  86. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    Am J Physiol Cell Physiol  2003;100:1322

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