U-73122

U-73122 Basic information
Product Name:U-73122
Synonyms:U-73122;1-[6-[[(17B)-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL]AMINO]HEXYL]-1H-PYRROLE-2,5-DIONE;1-[6-((17BETA-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL)AMINO)HEXYL]-1H-PYRROLE-2,5-DIONE;U-73122 98%;1-[6-[((17β)-3-methoxyestra-1,3,5[10]-trien-17-yl)amino]hexyl]-1h-pyrrole-2,5-dione;U-73122 hydrate;(17β)-3-Methoxy-17-[6-[(2,5-dihydro-2,5-dioxo-1H-pyrrol)-1-yl]hexylamino]estra-1,3,5(10)-triene;1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione
CAS:112648-68-7
MF:C29H40N2O3
MW:464.64
EINECS:
Product Categories:Lipid signaling;Inhibitors
Mol File:112648-68-7.mol
U-73122 Structure
U-73122 Chemical Properties
Boiling point 617.1±55.0 °C(Predicted)
density 1.16±0.1 g/cm3(Predicted)
storage temp. Keep in dark place,Inert atmosphere,Room temperature
solubility ethanol: 0.7 mg/mL
form solid
pka10.69±0.40(Predicted)
color off-white
Water Solubility Soluble in DMSO, ethanol, or DMF at approx. 0.5mg/ml. May require heating or overnight mixing. Insoluble in water
Stability:Stable for 1 year from date of purchase as supplied. Use caution when storing DMSO solutions. Typically solutions in DMSO can be stored at -20°C for approximately 2 months. However, any solutions that turn pink should be discarded.
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26-36
WGK Germany 3
MSDS Information
ProviderLanguage
SigmaAldrich English
U-73122 Usage And Synthesis
DescriptionU-73122 is an inhibitor of PLC-dependent processes, however, the mechanism of action remains unclear. The IC50 values for inhibition of platelet aggregation induced by collagen or thrombin are 0.6 and 5 μM, respectively. It also exhibits inhibitory activity against HIV-1 integrase with an IC50 value of 7 μM.
UsesIt is used as a phospholipase C, phospholipase A2, and 5-LO inhibitor. It is also determined that in SK-N-SH neuroblastoma cells, U-73122 inhibits agonist-induced down-regulation of muscarinic receptors. In addition, it is a useful tool to investigate receptor-mediated PI turnover in signal transduction. U-73122 is a potent inhibitor of human neutrophil adhesion to biological surfaces (IC50 = 50 nM) as well as adhesion-dependent granule exocytosis and oxidative burst. U-73343 (sc-201422) is useful as a negative control for investigations of U-73122 phospholipase C antagonism and its cellular consequences.
DefinitionChEBI: An aza-steroid that is 3-O-methyl-17beta-estradiol in which the 17beta-hydroxy group is replaced by a 6-(maleimid-1-yl)hexylamino group. An inibitor of phospholipase C.
Biological ActivityPhospholipase C inhibitor. Inhibits agonist-induced platelet aggregation with IC 50 values of 1-5 μ M. Potently inhibits human polymorphonuclear neutrophil adhesion on biological surfaces (IC 50 < 50 nM) and exhibits antinociceptive activity in vivo .
Biochem/physiol ActionsInhibits the hydrolysis of PPI to IP3, which leads to a decrease in cytosolic free calcium. Inhibits the coupling of G protein-phospholipase C activation, while remaining unaffected by production of cAMP.
storageStore at RT
References1) Bleasdale?et al. (1990),?Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils; J. Pharmacol. Exp. Ther.,?255?756 2) Zholos?et al.?(2004),?Phospholipase C, but not InsP3 or DAG,-dependent activation of the muscarinic receptor-operated cation current in guinea-pig ileal smooth muscle cells; Br. J. Pharmacol.,?141?23 3) Jun?et al. (2004),?Diacylglycerol and its formation by phospholipase C regulate Rab- and SNARE dependent yeast vacuole fusion; J. Biol. Chem. ,279?53186 4) Fernandez-Ulibarri?et al.?(2007),?Diacylglycerol is required for the formation of COPI vesicles in the Golgi-to-ER transport pathway; Mol. Biol. Cell,?18?3250
U-73122 Preparation Products And Raw materials
L-ALPHA-PHOSPHATIDYLINOSITOL LY 294002 HYDROCHLORIDE Ibrutinib 2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- Dasatinib Alpelisib (BYL719) U0126-EtOH Selumetinib Y27632 (hydrochloride) 3-METHYLADENINE 1-HEXYL-PYRROLE-2,5-DIONE U-73122

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