U-73122

• Description:

  U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  Ferroptosis; Lipoxygenase; Phospholipase

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; Metabolic Enzyme/Protease

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/u-73122.html

• Purity:

  99.79

• Solubility:

  DMSO : 5 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles:

  O=C (C=C1) N (CCCCCCN[C@H]2CC[C@@]3 ([H]) [C@]4 ([H]) CCC5=C (C=CC (OC) =C5) [C@@]4 ([H]) CC[C@]23C) C1=O

• Molecular Formula:

  C29H40N2O3

• Molecular Weight:

  464.64

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Smith RJ, et al. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. J Pharmacol Exp Ther. 1990 May;253 (2) :688-97.|[2]Bleasdale JE, et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther. 1990 Nov;255 (2) :756-68.|[3]Thompson AK, et al. The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation. J Biol Chem. 1991 Dec 15;266 (35) :23856-62.|[4]Peng T, et al. Disruption of phospholipase Cgamma1 signalling attenuates cardiac tumor necrosis factor-alpha expression and improves myocardial function during endotoxemia. Cardiovasc Res. 2008 Apr 1;78 (1) :90-7. Epub 2007 Dec 12.|[5]Frye CA, et al. In the ventral tegmental area, the membrane-mediated actions of progestins for lordosis of hormone-primed hamsters involve phospholipase C and protein kinase C. J Neuroendocrinol. 2007 Sep;19 (9) :717-24.|[6]Hörnig M, et al. Inhibition of 5-lipoxygenase by U73122 is due to covalent binding to cysteine 416. Biochim Biophys Acta. 2012 Feb;1821 (2) :279-86.|[7]Xie W, et al. 3Beta-hydroxy-6-aza-cholestane and related analogues as phosphatidylinositol specific phospholipase C (PI-PLC) inhibitors with antitumor activity. Bioorg Med Chem. 2000 Apr;8 (4) :699-706.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  5-LOX

• CAS Number:

  112648-68-7