PCSK9 Inhibitor, EGF-A

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).

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.

Primary Target
PCSK9

Packaged under inert gas

Toxicity: Standard Handling (A)

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

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

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

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