U 73122

Cat. No. 1268

U 73122 C29H40N2O3 [112648-68-7]

Price and Availability

For U 73122 pricing & availability please select your country from the drop down menu:
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 1-[6-[[(17β)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione

Biological Activity

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 U 73343 (Cat. No. 4133) also available.

Licensing Information

Sold with the permission of Pharmacia

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Select another batch:
Safety Data Sheet: View Safety Data Sheet

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

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for U 73122 include:

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

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

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.

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

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.

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.

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

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

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.

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

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

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.

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

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.

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.

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.

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

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

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.

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.

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

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

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.

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

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.

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.

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

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

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.

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.

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

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.

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.

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

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.

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

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

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

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.

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

Do you know of a great paper that uses U 73122 from Tocris? If so please let us know.show all ▼show less ▲

View Related Products by Product Action

Keywords: U 73122, supplier, Phospholipases, C, inhibitors, inhibits, PC-PLC, PI-PLC, Esterases, U73122, Tocris Bioscience, Phospholipase Inhibitor products

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Product Guide

Our Cancer Research Guide highlights over 750 products for cancer research. Request copy or view PDF today.

divider line

Cardiovascular Research Product Guide

Cardiovascular Research Product Guide

Our Cardiovascular Guide highlights over 250 products for cardiovascular research. Request copy or view PDF today.

divider line

New Therapies and Challenges in Asthma

Written by Peter J. Barnes

Asthma Life Science Poster

Our Asthma poster highlights key pathways and new therapies used to treat asthma, including those currently in clinical development. Request copy today.

divider line

New Products in this Area

XEN 445

Selective endothelial lipase inhibitor; orally bioavailable

Sign-up for new product e-alerts
divider line

LinkedIn Updates

Follow Tocris on LinkedIn

Follow us on LinkedIn!

Visit our LinkedIn page for the latest Tocris news, events and updates.