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508761 PCSK9 Inhibitor, EGF-A - Calbiochem

508761
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₈₈H₂₉₂N₅₈O₆₅S₆

Products

Catalogue NumberPackaging Qty/Pack
5.08761.0001 Glass bottle 1 mg
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
5.08761.0001 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.