Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  Metabolism >  Phospholipase (e.g. PLA) inhibitors >  U-73122

U-73122

Basic information Safety Supplier Related

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
Product Categories:
  • Lipid signaling
  • Inhibitors
Mol File:
112648-68-7.mol
More
Less

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
pka
10.69±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.
More
Less

Safety Information

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26-36
WGK Germany 
3

MSDS

More
Less

U-73122 Usage And Synthesis

Description

U-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.

Uses

It 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.

Definition

ChEBI: 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 Activity

Phospholipase 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 Actions

Inhibits 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.

storage

Store at RT

References

1) 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-73122Supplier

Zhengzhou convergence chemical co., LTD Gold
Tel
0371-0371-55153829 18003835034
Email
2853979819@qq.com
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Email
3bsc@sina.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn