579051 TAPI-1 - CAS 171235-71-5 - Calbiochem

579051
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₆H₃₇N₅O₅ 171235-71-5

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      579051-1MG
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          Plastic ampoule 1 mg
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          Description
          OverviewA structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α converting enzyme/ADAM17). TAPI-1 also blocks the shedding of several cell surface proteins such as IL-6 receptor, p60 TNF receptor, and p80 TNF receptor. Blocks constitutive (IC50 = 8.09 µM) and muscarinic receptor-stimulated (IC50 = 3.61 µM) sAAPα release in HEK 293 cells expressing M3 muscarinic receptors. A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579050) in DMSO is also available.
          Catalogue Number579051
          Brand Family Calbiochem®
          SynonymsN-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine, 2-aminoethyl Amide, TNF-α Protease Inhibitor-1
          References
          ReferencesSlack, B.E., et al. 2001. Biochem. J. 357, 787.
          Vincent, B., et al. 2001. J. Biol. Chem. 276, 37743.
          Hooper, N.M., et al. 1997. Biochem. J. 321, 265.
          Crowe, P.D., et al. 1995. J. Exp. Med. 181, 1205.
          Mullberg, J., et al. 1995. J. Immunol. 155, 5198.
          Mohler, K.M., et al. 1994. Nature 370, 218.
          Product Information
          CAS number171235-71-5
          ATP CompetitiveN
          DeclarationManufactured exclusively by Peptides International, Louisville, Kentucky, USA.
          FormWhite solid
          Hill FormulaC₂₆H₃₇N₅O₅
          Chemical formulaC₂₆H₃₇N₅O₅
          Hygroscopic Hygroscopic
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetMMPs and TACE
          Primary Target IC<sub>50</sub>8.09 µM and 3.61 µM blocking constitutive and muscarinic receptor-stimulated sAAPα release in HEK 293 cells expressing M3 muscarinic receptors, respectively
          Purity≥97% by HPLC
          Physicochemical Information
          Cell permeableN
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage -20°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          TAPI-1 - CAS 171235-71-5 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          TAPI-1 - CAS 171235-71-5 - Calbiochem Certificates of Analysis

          TitleLot Number
          579051

          References

          Reference overview
          Slack, B.E., et al. 2001. Biochem. J. 357, 787.
          Vincent, B., et al. 2001. J. Biol. Chem. 276, 37743.
          Hooper, N.M., et al. 1997. Biochem. J. 321, 265.
          Crowe, P.D., et al. 1995. J. Exp. Med. 181, 1205.
          Mullberg, J., et al. 1995. J. Immunol. 155, 5198.
          Mohler, K.M., et al. 1994. Nature 370, 218.

          Citations

          Title
        • Daniel W. Lambert, et al. (2005) Tumor Necrosis Factor- Convertase (ADAM17) Mediates Regulated Ectodomain Shedding of the Severe-acute Respiratory Syndrome-Coronavirus (SARS-CoV) Receptor, Angiotensin-converting Enzyme-2 (ACE2). Journal of Biological Chemistry 280, 30113-30119.
        • Daniel W. Lambert, et al. (2005) Tumor necrosis factor-alpha convertase (ADAM17) mediates regulated ectodomain shedding of the SARS-CoV receptor, angiotensin-converting enzyme-2 (ACE2). Journal of Biological Chemistry 280, 30113-30119.
        • Xu-Wen Liu, et al. (2005) Tissue inhibitor of metalloproteinase-1 protects human breast epithelial cells from extrinsic cell death: a potential oncogenic activity of tissue inhibitor of metalloproteinase-1. Cancer Research 65, 898-906.
        • Evelyn Roth and Hanspeter Pircher. (2004) IFN-γ promotes Fas ligand- and perforin-mediated liver cell destruction by cytotoxic CD8 T cells. Journal of Immunology 172, 1588-1594.
        • 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.

          Revision04-April-2011 RFH
          SynonymsN-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine, 2-aminoethyl Amide, TNF-α Protease Inhibitor-1
          DescriptionA structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α convertase; ADAM17). However, TAPI-1 is more stable in serum than TAPI-0. TAPI-1 Blocks the shedding of several cell surface proteins such as TNF-α, IL-6 receptor, and p60 and p80 TNF receptors. Inhibits constitutive (IC50 = 8.09 µM) and muscarinic receptor-stimulated (IC50 = 3.61 µM) sAPPa release in HEK-293 cells expressing muscarinic receptors. Also blocks the TACE-dependent constitutive release of co-transfected APP(695) (IC50 = 920 nM).
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number171235-71-5
          Chemical formulaC₂₆H₃₇N₅O₅
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (5 mg/ml) or Methanol (1 mg/ml)
          Storage -20°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
          Toxicity Standard Handling
          ReferencesSlack, B.E., et al. 2001. Biochem. J. 357, 787.
          Vincent, B., et al. 2001. J. Biol. Chem. 276, 37743.
          Hooper, N.M., et al. 1997. Biochem. J. 321, 265.
          Crowe, P.D., et al. 1995. J. Exp. Med. 181, 1205.
          Mullberg, J., et al. 1995. J. Immunol. 155, 5198.
          Mohler, K.M., et al. 1994. Nature 370, 218.
          Citation
        • Daniel W. Lambert, et al. (2005) Tumor Necrosis Factor- Convertase (ADAM17) Mediates Regulated Ectodomain Shedding of the Severe-acute Respiratory Syndrome-Coronavirus (SARS-CoV) Receptor, Angiotensin-converting Enzyme-2 (ACE2). Journal of Biological Chemistry 280, 30113-30119.
        • Daniel W. Lambert, et al. (2005) Tumor necrosis factor-alpha convertase (ADAM17) mediates regulated ectodomain shedding of the SARS-CoV receptor, angiotensin-converting enzyme-2 (ACE2). Journal of Biological Chemistry 280, 30113-30119.
        • Xu-Wen Liu, et al. (2005) Tissue inhibitor of metalloproteinase-1 protects human breast epithelial cells from extrinsic cell death: a potential oncogenic activity of tissue inhibitor of metalloproteinase-1. Cancer Research 65, 898-906.
        • Evelyn Roth and Hanspeter Pircher. (2004) IFN-γ promotes Fas ligand- and perforin-mediated liver cell destruction by cytotoxic CD8 T cells. Journal of Immunology 172, 1588-1594.