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662035

Sigma-Aldrich

U-73122

≥98% (HPLC), solid, agonist-induced phospholipase C activation inhibitor, Calbiochem®

Sinonimo/i:

U-73122, 1-[6-((17β-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl]-1H-pyrrole-2,5-dione

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About This Item

Formula empirica (notazione di Hill):
C29H40N2O3
Numero CAS:
Peso molecolare:
464.64
Codice UNSPSC:
41121800
NACRES:
NA.77

product name

U-73122, U-73122, CAS 112648-68-7, inhibits agonist-induced phospholipase C activation (IC50 = 1-2.1 µM) in human platelets and neutrophils.

Livello qualitativo

Saggio

≥98% (HPLC)

Forma fisica

solid

Produttore/marchio commerciale

Calbiochem®

Condizioni di stoccaggio

OK to freeze

Colore

off-white

Solubilità

anhydrous DMSO: 1 mg/mL
chloroform: 3 mg/mL
anhydrous ethanol: 500 μg/mL

Condizioni di spedizione

ambient

Temperatura di conservazione

10-30°C

InChI

1S/C29H40N2O3/c1-29-16-15-23-22-10-8-21(34-2)19-20(22)7-9-24(23)25(29)11-12-26(29)30-17-5-3-4-6-18-31-27(32)13-14-28(31)33/h8,10,13-14,19,23-26,30H,3-7,9,11-12,15-18H2,1-2H3/t23-,24-,25+,26+,29+/m1/s1
LUFAORPFSVMJIW-ZRJUGLEFSA-N

Descrizione generale

A potent, selective, and cell-permeable inhibitor C-type phosphatidylinositol-specific phospholipases. Inhibits agonist-induced phospholipase C activation (IC50 = 1-2.1 µM) in human platelets and neutrophils. Inhibits ET-1 and parathyroid hormone induced Ca2+ transients (IC50 = 800 nM and 500 nM, respectively). Also inhibits agonist-induced down-regulation of muscarinic receptors in SK-N-SH neuroblastoma cells. Acts as a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces (IC50 = 50 nM). Abolishes T lymphoma cell invasion into fibroblast monolayers.
A potent, selective, and cell-permeable inhibitor C-type phosphatidylinositol-specific phospholipases. Inhibits agonist-induced phospholipase C activation (IC50 = 1-2.1 µM) in human platelets and neutrophils. Inhibits ET-1 and parathyroid hormone-induced Ca2+ transients (IC50 = 800 nM and 500 nM, respectively). Also inhibits agonist-induced down-regulation of muscarinic receptors in SK-N-SH neuroblastoma cells. Acts as a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces (IC50 = 50 nM). Reported to abolish T lymphoma cell invasion into fibroblast monolayers.

Azioni biochim/fisiol

Cell permeable: yes
Primary Target
Agonist-induced phospholipase C activation
Product does not compete with ATP.
Reversible: no
Target IC50: 1-2.1 µM against agonist-induced phospholipase C activation in human platelets and neutrophils; 800 nM and 500 nM, respectively, against ET-1 and parathyroid hormone-induced Ca2+ transients; 50 nM against human polymorphonuclear neutrophil adhesion

Attenzione

Toxicity: Irritant (B)

Nota sulla preparazione

The use of anhydrous solvents is critical for the solubility of the compound; the presence of moisture in the solvent will lower the solubility of the compound.

Ricostituzione

Unstable in DMSO and ethanol; reconstitute in anhydrous DMSO or ethanol just prior to use. Following reconstitution in anhydrous chloroform, aliquot into single use volumes, evaporate to dryness under a stream of nitrogen, and freeze (-20°C. Dried aliquots are stable for up to 6 months at -20°C. ); Reconstitute dried aliquots in anhydrous DMSO or anhydrous ethanol just prior to use.

Altre note

Stam, J.C., et al. 1998. EMBO J. 17, 4066.
Smith, R.J., et al. 1996. J. Pharmacol. Exp. Ther.278, 320.
Tatrai, A., et al. 1994. Biochim. Biophys. Acta 1224, 595.
Wang, X.D., et al. 1994. Biochim. Biophys. Acta1223, 101.
Bleasdale, J.E., and Fisher, S.K. 1993. Neuroprotocols: A Companion to Methods in Neurosci. 3, 125.
Wu, H., et al. 1992. Biochemistry31, 3370.
Yule, D.I., and Williams, J.A. 1992. J. Biol. Chem.267, 13830.
Thompson, A.K., et al. 1991. J. Biol. Chem.266, 23856.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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