508761 | PCSK9 Inhibitor, EGF-A - Calbiochem

508761
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₈₈H₂₉₂N₅₈O₆₅S₆

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.08761.0001
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          Glass bottle 1 mg
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          Description
          OverviewA 42-mer synthetic peptide (GTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDI-NH2) that contains a calcium binding site of EGF-A. Binds to the proprotein convertase subtilisin/kexin type 9 (PCSK9) in a pH and calcium-dependent manner (Kd = 300 nM at pH 5.2 and 1.0 µM at pH7.4 and at 2 mM calcium) and blocks its interaction with LDL receptors (IC50 = 3.4 µM) and VLDL receptors (IC50 = 4.7 µM). Acts as a poor inhibitor of PCSK9 - Apo-ER2 interaction even at high concentrations (~200 µM). Blocks the degradation of mature LDL receptors in HepG2 cells in a dose-dependent manner (~1.5 to 15 µM).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number508761
          Brand Family Calbiochem®
          References
          ReferencesShan L, et al. 2008. Biochem Biophys Res Commun. 375, 69.
          Da-Wei Zhang, et al. 2007. J. Biol. Chem. 282, 18602.
          Product Information
          FormWhite powder
          Hill FormulaC₁₈₈H₂₉₂N₅₈O₆₅S₆
          Chemical formulaC₁₈₈H₂₉₂N₅₈O₆₅S₆
          Hygroscopic Hygroscopic
          Applications
          Biological Information
          Primary TargetPCSK9
          Primary Target K<sub>i</sub>0.3 µ
          Purity≥95% by HPLC
          Physicochemical Information
          Peptide SequenceGTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDI-NH2 (Disulfide Bridge: 5-16, 12-25, 27-39)
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Shan L, et al. 2008. Biochem Biophys Res Commun. 375, 69.
          Da-Wei Zhang, et al. 2007. J. Biol. Chem. 282, 18602.

          Brochure

          Title
          NPI Flyer- Epigenetics and Nuclear Function Feature (EMD)
          New Products - Antibodies, Small Molecule, Inhibitors

          Technical Info

          Title
          White Paper: Further considerations of antibody validation and usage. (EMD)
          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.

          Revision19-December-2014 JSW
          DescriptionA 42-mer synthetic peptide (GTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDI-NH2) that contains a calcium binding site of EGF-A. Binds to the proprotein convertase subtilisin/kexin type 9 (PCSK9) in a pH and calcium-dependent manner (Kd = 300 nM at pH 5.2 and 1.0 µM at pH7.4 and at 2 mM calcium) and blocks its interaction with LDL receptors (IC50 = 3.4 µM) and VLDL receptors (IC50 = 4.7 µM). Acts as a poor inhibitor of PCSK9 - Apo-ER2 interaction even at high concentrations (~200 µM). Blocks the degradation of mature LDL receptors in HepG2 cells in a dose-dependent manner (~1.5 to 15 µM).
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₈₈H₂₉₂N₅₈O₆₅S₆
          Peptide SequenceGTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDI-NH2 (Disulfide Bridge: 5-16, 12-25, 27-39)
          Purity≥95% by HPLC
          SolubilityH₂O (25 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesShan L, et al. 2008. Biochem Biophys Res Commun. 375, 69.
          Da-Wei Zhang, et al. 2007. J. Biol. Chem. 282, 18602.