Replaces Prod. #: ALX-370-005
Inhibits agonist induced phospholipase C (PLC) activation (IC50=1-2.1 µM) in human platelets. It also inhibits agonist induced down-regulation of muscarinic receptors in SK-N-SH neuroblastoma cells. It is a useful tool to investigate receptor-mediated PI turnover in signal transduction. It is a potent inhibitor of human neutrophil adhesion to biological surfaces as well as adhesion-dependent granule exocytosis and oxidative burst. Inhibits 5-lipoxygenase in vivo and in vitro (IC50 = 30nM for recombinant enzyme and 2.4µM for PMNL homogenates).
Product Details
| Alternative Name: | 1-(6-((17β-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione |
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| Formula: | C29H40N2O3 |
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| MW: | 464.7 |
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| CAS: | 112648-68-7 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | white to off-white solid |
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| Solubility: | Soluble in methylene chloride or chloroform. Slightly soluble in DMSO (2mg/ml) or 100% ethanol (1mg/ml), sparingly soluble in aqueous solutions. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | Ambient |
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| Use/Stability: | U73122 is only sparingly soluble in aqueous media. Therefore the compounds are delivered to cells either after dissolving in organic solvents or complexing with serum proteins. Serum albumin (1-10mg/ml).
Dissolve a weighed amount of U-73122 in methylene chloride or chloroform. Dispense in aliquots sufficient for one experiment into suitable vessels. Evaporate solvent with nitrogen.
Stock solutions in DMSO or ethanol are stable for 2 months when stored at -20°C. Preferably dissolve just before use. Use caution in reusing stored DMSO solutions. Discard solutions that have turned to a pink color, which indicates a loss of inhibitor activity. Dried aliquots prepared from chloroform solutions are stable for up to 1 month when stored at -20°C.
Useful range of concentrations for U-73122 is 0.1 to 10μM. The appropriate concentration will depend upon the cell type, cell density, medium concentration (the maleimide moiety of U-73122 may react with thiol containing compounds) and the particular cell parameter that is being measured.
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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The aminosteroid phospholipase C antagonist U-73122 (1-[6-[[17-beta-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrro le-2,5-dione) potently inhibits human 5-lipoxygenase in vivo and in vitro: C. Feisst, et al.; Mol. Pharmacol.
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U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions: R.J. Smith, et al.; J. Pharmacol. Exp. Ther.
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A phospholipase C inhibitor, U-73122, blocks TSH-induced inositol trisphosphate production, Ca2+ increase and arachidonic acid release in FRTL-5 thyroid cells: X.D. Wang, et al.; Biochim. Biophys. Acta
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U-73122, a phospholipase C antagonist, inhibits effects of endothelin-1 and parathyroid hormone on signal transduction in UMR-106 osteoblastic cells: A. Tatrai, et al.; Biochim. Biophys. Acta
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Use of U-73122 as an Inhibitor of Phospholipase C-Dependent Processes: J.E. Bleasdale & S.K. Fisher; Neuroprotocols
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U-73122, an aminosteroid phospholipase C antagonist, noncompetitively inhibits thyrotropin-releasing hormone effects in GH3 rat pituitary cells: R.C. Smallridge, et al.; Endocrinology
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