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Merck
CN

5.08761

PCSK9 Inhibitor, EGF-A

Synonym(s):

PCSK9 Inhibitor, EGF-A

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About This Item

Empirical Formula (Hill Notation):
C188H292N58O65S6
Molecular Weight:
4597.07
NACRES:
NA.77
UNSPSC Code:
12352200

Key Documents

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assay

≥95% (HPLC)

form

powder

potency

0.3 μM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

white

solubility

water: 25 mg/mL

storage temp.

−20°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Primary Target
PCSK9

Disclaimer

Toxicity: Standard Handling (A)

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 (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.

Other Notes

GTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDI-NH2 (Disulfide Bridge: 5-16, 12-25, 27-39)
Shan L, et al. 2008. Biochem Biophys Res Commun.375, 69.
Da-Wei Zhang, et al. 2007. J. Biol. Chem.282, 18602.

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

新产品
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Certificates of Analysis (COA)

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