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508761 PCSK9 Inhibitor, EGF-A - Calbiochem

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₈₈H₂₉₂N₅₈O₆₅S₆

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5087610001
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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5087610001 04055977261387

      Documentation

      PCSK9 Inhibitor, EGF-A - Calbiochem 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
      New Products - Antibodies, Small Molecule, Inhibitors

      Technical Info

      Title
      White Paper: Further considerations of antibody validation and usage.
      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 Protect from light
      -20°C
      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.
      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.