662035

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
• Formula empirica (notazione di Hill): C₂₉H₄₀N₂O₃
• Numero CAS: 112648-68-7
• Peso molecolare: 464.64
• Numero MDL: MFCD00893825
• Codice UNSPSC: 41121800
• NACRES: NA.77

Proprietà

• Nome del prodotto: 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: 100
• Saggio: ≥98% (HPLC)
• Stato: 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
• Stringa SMILE: N5(C(=O)C=CC5=O)CCCCCCN[C@@H]1[C@@]2([C@H]([C@H]3[C@H](CC2)c4c(cc(cc4)OC)CC3)CC1)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

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). 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

Informazioni sulla sicurezza

• 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