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

662035
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₉H₄₀N₂O₃ 112648-68-7

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      662035-5MG
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          Plastic ampoule 5 mg
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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
          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

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          U-73122 - CAS 112648-68-7 - Calbiochem Certificates of Analysis

          TitleLot Number
          662035

          References

          Reference overview
          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

          Title
        • 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,.
        • Data Sheet

          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,.