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U-73122

Inhibitor of PLC activation
 
BML-ST391-0005 5 mg 93.00 USD
 
BML-ST391-0025 25 mg 367.00 USD
Do you need bulk/larger quantities?
 
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 Specification

Alternative Name:1-(6-((17β-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione
 
Formula:C29H40N2O3
 
MW:464.7
 
CAS:112648-68-7
 
Purity:≥98% (HPLC)
 
Appearance:white to off-white solid
 
Solubility:Soluble in methylene chloride or chloroform. Slightly soluble in DMSO (2mg/ml) or 100% ethanol (1mg/ml), sparingly soluble in aqueous solutions. 
 
Shipping:Ambient
 
Long Term Storage:Ambient
 
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.
 
BML-ST391 structure
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BML-ST391 structure

Product Literature References

VLDL-activated cell signaling pathways that stimulate adrenal cell aldosterone production: Y.Y. Tsai, et al.; Mol. Cell. Endocrinol. 433, 138 (2016), Application(s): Cell culture, Abstract;
Activation of phosphatidylinositol 3-kinase β by the platelet collagen receptors integrin α2β1 and GPVI: The role of Pyk2 and c-Cbl: D. Manganaro, et al.; Biochim. Biophys. Acta 1853, 1879 (2015), Application(s): Cell Culture, Abstract;
CXCL12 regulates platelet activation via the regulator of G-protein signaling 16: Z.A. Karim, et al.; Biochim. Biophys. Acta 1863, 314 (2015), Application(s): Cell culture, Abstract;
FGF9-induced changes in cellular redox status and HO-1 upregulation are FGFR-dependent and proceed through both ERK and AKT to induce CREB and Nrf2 activation: J.I. Chuang, et al.; Free Radic. Biol. Med. 89, 274 (2015), Application(s): Cell Culture, Abstract;
Serine-727 phosphorylation activates hypothalamic STAT-3 independently from tyrosine-705 phosphorylation: A. Breit, et al.; Mol. Endocrinol. 29, 445 (2015), Application(s): ELISA, Abstract; Full Text
Comparative Effects of the Endogenous Agonist Glucagon-Like Peptide-1 (GLP-1)-(7-36) Amide and the Small-Molecule Ago-Allosteric Agent "Compound 2" at the GLP-1 Receptor: K. Coopman, et al.; J. Pharmacol. Exp. Ther. 334, 795 (2010), Application(s): IP of human embryonic kidney cells, Abstract; Full Text
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. 67, 1751 (2005), Abstract;
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. 278, 320 (1996), Abstract;
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 1223, 101 (1994), Abstract;
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 1224, 575 (1994), Abstract;
Use of U-73122 as an Inhibitor of Phospholipase C-Dependent Processes: J.E. Bleasdale & S.K. Fisher; Neuroprotocols 3, 125 (1993), Full Text
U-73122, an aminosteroid phospholipase C antagonist, noncompetitively inhibits thyrotropin-releasing hormone effects in GH3 rat pituitary cells: R.C. Smallridge, et al.; Endocrinology 131, 1883 (1992), Abstract;
U73122 inhibits Ca2+ oscillations in response to cholecystokinin and carbachol but not to JMV-180 in rat pancreatic acinar cells: D.I. Yule, et al.; J. Biol. Chem. 267, 13830 (1992), Abstract;
The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation: A.K. Thompson, et al.; J. Biol. Chem. 266, 23856 (1991), Abstract;
Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness: R.J. Smith, et al.; J. Pharmacol. Exp. Ther. 253, 688 (1990), Abstract;
Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils: J.E. Bleasdale, et al.; J. Pharmacol. Exp. Ther. 255, 756 (1990), Abstract;

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