Cat. # AG-CR1-3698

Product Details

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

 

Properties

Formula                    C29H40N2O3

MW                          464.6

CAS                         112648-68-7

RTECS                     UX9626600

Purity Chemicals      ≥95%

Appearance             White to off-white solid.

Solubility                  Soluble in methylene chloride or chloroform (10mg/ml).

                                 Slightly soluble in DMSO (2mg/ml), DMF (2mg/ml) or 100%                                   ethanol (1mg/ml). Sparingly soluble in aqueous solutions.

                                 See also Solubility Note below.

Other Product          Solubility/Stability and Application NOTE:

Data                          U-73122 is only sparingly soluble in aqueous media. 

                                 Therefore the compound is delivered to cells either after 

                                 dissolving in organic solvents or complexing with serum

                                 proteins.

Preparation of a Working solution:

  1. Dissolve a weighed amount of U-73122 in methylene chloride or  chloroform.

  2. Dispense in aliquots sufficient for one  experiment into suitable vessels.         

      Evaporate solvent with nitrogen.

  3. The resulting film can be dissolved in DMSO (5mM), ethanol (2mM in 100%)

      or an aqueous medium that contains serum or serum albumin (1-10 mg/ml),

      which forms a complex with U-73122, thus eliminating the need to use an

      organic solvent to deliver the compound to the cells.

Stability:

  Stock solutions in DMSO or ethanol are stable for 2 months when stored at 

  -20°C. Preferably dissolve just before use. Use caution in re-using 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.

Application:

  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.

InChi Key                  LUFAORPFSVMJIW-ZRJUGLEFSA-N

Smiles    C[C@@]12[C@](CC[C@@H]2NCCCCCCN3C(C=CC3=O)=O)([H])[C@]4([H])CCC5=CC(OC)=CC=C5[C@@]4([H])CC1

Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Protect from light.
Protect from moisture.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.

U-73122

    • Gasdermin D N-terminal fragment (GSDMD-N)-induced pyroptosis inhibitor. Protects against GSDMD-N cytotoxicity in macrophages or against lethal infection in mice.
    • Useful agent for inflammasome research.
    • Potent cell permeable phospholipase C (PLC) , phospholipase A2 and 5-LO (5-lipoxygenase) inhibitor. Affects the phospholipases by inhibiting the hydrolysis of PPI (phosphatidylinositol) to IP3 (inositol triphosphate), which in turn leads to a drop in cytosolic Ca2+.
    • Potent inhibitor of the SERCA pump in smooth muscle. Potently inhibits Ca2+-release from isolated smooth muscle cells independent of its effect on PLC.
    • Inhibits agonist-induced platelet aggregation. Potently inhibits human polymorphonuclear neutrophil adhesion on biological surfaces and exhibits antinociceptive activity in vivo. Shown to inhibit agonist-induced down-regulation of muscarinic receptors in SK-N-SH neuroblastoma cells.
    • Activates TRPM4 and inhibits TRPM3 channels.
    • Potent human telomerase inhibitor.

    Product References

    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)

    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)

    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)

    Use of U-73122 as an Inhibitor of Phospholipase C-Dependent Processes: J.E. Bleasdale & S.K. Fisher; Neuroprotocols 3, 125 (1993)

    Calcium homeostasis in mouse fibroblast cells: affected by U-73122, a putative phospholipase C beta blocker, via multiple mechanisms: J.P. Grierson & J. Meldolesi; Br. J. Pharmacol. 115, 11 (1995)

    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)

    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)

    Potent inhibition of human telomerase by U-73122: Y.J. Chen, et al.; J. Biomed. Sci. 13, 667 (2006)

    The PI-PLC inhibitor U-73122 is a potent inhibitor of the SERCA pump in smooth muscle: M.A. Hollywood, et al.; Br. J. Pharmacol. 160, 1293 (2010)

    VLDL-activated cell signaling pathways that stimulate adrenal cell aldosterone production: Y.Y. Tsai, et al.; Mol. Cell. Endocrinol. 433, 138 (2016)

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

    Lipid peroxidation drives Gasdermin D-mediated pyroptosis in lethal polymicrobial Sepsis: R. Kang, et al.; Cell Host Microbe 24, 97 (2018)

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