U-73122

Bezeichnung:U-73122

CAS-Nr112648-68-7

Englisch Name:U-73122

CBNumberCB6237598

SummenformelC29H40N2O3

Molgewicht464.64

MOL-Datei112648-68-7.mol

U-73122 physikalisch-chemischer Eigenschaften

Siedepunkt	617.1±55.0 °C(Predicted)
Dichte	1.16±0.1 g/cm3(Predicted)
storage temp.	Keep in dark place,Inert atmosphere,Room temperature
Löslichkeit	ethanol: 0.7 mg/mL
Aggregatzustand	solid
pka	10.69±0.40(Predicted)
Farbe	off-white
Wasserlöslichkeit	Soluble in DMSO, ethanol, or DMF at approx. 0.5mg/ml. May require heating or overnight mixing. Insoluble in water
Stabilität	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.

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36
WGK Germany	3

Gefahreninformationscode (GHS)

U-73122 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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.
Verwenden
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.
Biologische Aktivität
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.
Lager
Store at RT
Einzelnachweise
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-73122 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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