U 73122

Pricing Availability Delivery Time Qty
Cat.No. 1268 - U 73122 | C29H40N2O3 | CAS No. 112648-68-7
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)
Datasheet
Citations (48)
Literature

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

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.32 5mM with gentle warming
ethanol 0.93 2

Preparing Stock Solutions

The following data is based on the product molecular weight 464.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.15 mL 10.76 mL 21.52 mL
5 mM 0.43 mL 2.15 mL 4.3 mL
10 mM 0.22 mL 1.08 mL 2.15 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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: 7328745


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

View Related Products by Product Action

View all Phospholipase Inhibitors

Keywords: Phospholipases C inhibitors inhibits PC-PLC PI-PLC Esterases U73122 Phospholipases

48 Citations for U 73122

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

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

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

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

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) Dopamine Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation. PLoS One 10 e0124986 PMID: 25938462

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Asthma

Asthma Poster

Asthma is one of the most common chronic diseases in the world, affecting over 300 million people. This poster highlights key pathways and new therapies used to treat the condition, including those currently in clinical development.

Pathways for U 73122

Protocols

TODO: Add Protocols