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
Assay:
≥95% (HPLC)
Form:
powder
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Pricing and availability is not currently available.
assay
≥95% (HPLC)
Quality Segment
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
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
PCSK9
PCSK9
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.
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.
Da-Wei Zhang, et al. 2007. J. Biol. Chem.282, 18602.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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This Item | |||
|---|---|---|---|
| form powder | form solid | form lyophilized solid | form solid |
| assay ≥95% (HPLC) | assay ≥95% (HPLC) | assay ≥97% (HPLC) | assay ≥97% (HPLC) |
| manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level 100 |
| storage temp. −20°C | storage temp. 2-8°C | storage temp. −20°C | storage temp. −20°C |
| solubility water: 25 mg/mL | solubility DMSO: 100 mg/mL, ethanol: 5 mg/mL | solubility water: 5 mg/mL | solubility ethanol: 25 mg/mL, DMSO: 50 mg/mL |
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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