5.08761

PCSK9 Inhibitor, EGF-A

• Synonym(s): PCSK9 Inhibitor, EGF-A
• Empirical Formula (Hill Notation): C₁₈₈H₂₉₂N₅₈O₆₅S₆
• Molecular Weight: 4597.07
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥95% (HPLC)
• Quality Level: 100
• form: powder
• potency: 0.3 μM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: water: 25 mg/mL
• storage temp.: −20°C

Description

General description

A 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 (K_d = 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.

Biochem/physiol Actions

Primary Target
PCSK9

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

GTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDI-NH2 (Disulfide Bridge: 5-16, 12-25, 27-39)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable