662035
U-73122
≥98% (HPLC), solid, agonist-induced phospholipase C activation inhibitor, Calbiochem®
Synonyme(s) :
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
Formule empirique (notation de Hill):
C29H40N2O3
Numéro CAS:
Poids moléculaire :
464.64
Code UNSPSC :
41121800
Nomenclature NACRES :
NA.77
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Nom du produit
U-73122, U-73122, CAS 112648-68-7, inhibits agonist-induced phospholipase C activation (IC50 = 1-2.1 µM) in human platelets and neutrophils.
Niveau de qualité
Essai
≥98% (HPLC)
Forme
solid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
Couleur
off-white
Solubilité
anhydrous DMSO: 1 mg/mL
chloroform: 3 mg/mL
anhydrous ethanol: 500 μg/mL
Conditions d'expédition
ambient
Température de stockage
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
Clé InChI
LUFAORPFSVMJIW-ZRJUGLEFSA-N
Description générale
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.
Actions biochimiques/physiologiques
Cell permeable: yes
Primary Target
Agonist-induced phospholipase C activation
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
Avertissement
Toxicity: Irritant (B)
Notes préparatoires
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.
Reconstitution
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.
Autres remarques
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.
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.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".
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