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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 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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
662035
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
112648-68-7C₂₉H₄₀N₂O₃

Products

Catalogue NumberPackaging Qty/Pack
662035-5MG Plastic ampoule 5 mg
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
Catalogue Number GTIN
662035-5MG 07790788052256

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,.
    		•