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662035 U-73122 - CAS 112648-68-7 - Calbiochem

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

U-73122 - CAS 112648-68-7 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

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

Primary Target: Agonist-induced phospholipase C activation
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662035
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Tableau de caractéristiques principal

CAS #Empirical Formula
112648-68-7C₂₉H₄₀N₂O₃

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      Description
      OverviewA 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.
      Catalogue Number662035
      Brand Family Calbiochem®
      Synonyms1-[6-((17β-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl]-1H-pyrrole-2,5-dione
      References
      ReferencesStam, 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. Acta 1223, 101.
      Bleasdale, J.E., and Fisher, S.K. 1993. Neuroprotocols: A Companion to Methods in Neurosci. 3, 125.
      Wu, H., et al. 1992. Biochemistry 31, 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.
      Product Information
      CAS number112648-68-7
      ATP CompetitiveN
      FormOff-white solid
      Hill FormulaC₂₉H₄₀N₂O₃
      Chemical formulaC₂₉H₄₀N₂O₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationU-73122, CAS 112648-68-7, inhibits agonist-induced phospholipase C activation (IC50 = 1-2.1 µM) in human platelets and neutrophils.
      Biological Information
      Primary TargetAgonist-induced phospholipase C activation
      Primary Target IC<sub>50</sub>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
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 36/37/38

      Irritating to eyes, respiratory system and skin.
      S PhraseS: 26-36

      In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
      Wear suitable protective clothing.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Irritant
      Storage +15°C to +30°C
      Do not freeze Ok to freeze
      Special InstructionsUnstable 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.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      662035-5MG 07790788052256

      Documentation

      U-73122 - CAS 112648-68-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      U-73122 - CAS 112648-68-7 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      662035

      Références bibliographiques

      Aperçu de la référence bibliographique
      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. Acta 1223, 101.
      Bleasdale, J.E., and Fisher, S.K. 1993. Neuroprotocols: A Companion to Methods in Neurosci. 3, 125.
      Wu, H., et al. 1992. Biochemistry 31, 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.

      Citations

      Titre
    • M. Keith Wilkerson, et al. (2006) Inositol triphosphate receptor calcium release is required for cerebral artery smooth muscle cell proliferation. American Journal of Physiology Heart and Circulatory Physiology 290, H240-H247.
    • Martha E. O'Donnnell, et al. (2005) Arginine Vasopressin Stimulation of Cerebral Microvascular Endothelial Cell Na-K-Cl Cotransporter Activity is V1 Receptor and [Ca] Dependent. American Journal of Physiology Cell Physiology 289, C283-C292.
    • Di Zhang, et al. (2005) Strontium Promotes Calcium Oscillations in Mouse Meiotic Oocytes and Early Embryos Through InsP3 Receptors, and Requires Activation of Phopsholipase and the Synertistic Action of InsP3. Human Reproduction in press,.
      		•
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision18-August-2017 JSW
      Synonyms1-[6-((17β-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl]-1H-pyrrole-2,5-dione
      DescriptionA 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.
      FormOff-white solid
      CAS number112648-68-7
      Chemical formulaC₂₉H₄₀N₂O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityAnhydrous Chloroform (3 mg/ml), Anhydrous DMSO (1 mg/ml), or Anhydrous Ethanol (500 µg/ml). 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.
      Storage +15°C to +30°C
      Do Not Freeze Ok to freeze
      Special InstructionsUnstable 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.
      Toxicity Irritant
      ReferencesStam, 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. Acta 1223, 101.
      Bleasdale, J.E., and Fisher, S.K. 1993. Neuroprotocols: A Companion to Methods in Neurosci. 3, 125.
      Wu, H., et al. 1992. Biochemistry 31, 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.
      Citation
    • M. Keith Wilkerson, et al. (2006) Inositol triphosphate receptor calcium release is required for cerebral artery smooth muscle cell proliferation. American Journal of Physiology Heart and Circulatory Physiology 290, H240-H247.
    • Martha E. O'Donnnell, et al. (2005) Arginine Vasopressin Stimulation of Cerebral Microvascular Endothelial Cell Na-K-Cl Cotransporter Activity is V1 Receptor and [Ca] Dependent. American Journal of Physiology Cell Physiology 289, C283-C292.
    • Di Zhang, et al. (2005) Strontium Promotes Calcium Oscillations in Mouse Meiotic Oocytes and Early Embryos Through InsP3 Receptors, and Requires Activation of Phopsholipase and the Synertistic Action of InsP3. Human Reproduction in press,.
      		•