|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 Data||
Solubility/Stability and Application NOTE:
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:
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
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.|
|Product Specification Sheet|
- 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.
- 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)