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SML1132

Sigma-Aldrich

Pep2-8 trifluoroacetate salt

≥95% (HPLC), contains 58μL of solution at 10mM in DMSO

Synonym(s):

Ac-TVFTSWEEYLDWV-NH2 trifluoroacetate salt, Ac-TVFTSWEEYLDWV-amide trifluoroacetate salt, Ac-Thr-Val-Phe-Thr-Ser-Trp-Glu-Glu-Tyr-Leu-Asp-Trp-Val-NH2 trifluoroacetate salt

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About This Item

Empirical Formula (Hill Notation):
C83H110N16O24 · xC2HF3O2
Molecular Weight:
1715.85 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥95% (HPLC)

form

solution

color

colorless to pale yellow

shipped in

wet ice

storage temp.

−20°C

Amino Acid Sequence

Ac-Thr-Val-Phe-Thr-Ser-Trp-Glu-Glu-Tyr-Leu-Asp-Trp-Val-NH2 trifluoroacetate salt

Biochem/physiol Actions

Pep2-8 is a potent PCSK9 (proprotein convertase subtilisin/kexin type 9) inhibitor that selectively binds to PCSK9 and interferes with LDL receptor binding to PCSK9. Pep2-8 restores LDL receptor function and LDL uptake of PCSK9-treated HepG2 cells.
Pep2-8, a good mimic of epidermal growth factor precursor homology domain A (EGF-A), serves as a competitive inhibitor of low-density lipoprotein (LDL) receptor binding. It can be used as an anchor peptide in phage-display experiments to bind an extension peptide library to the groove site.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Yingnan Zhang et al.
The Journal of biological chemistry, 289(2), 942-955 (2013-11-15)
PCSK9 (proprotein convertase subtilisin/kexin type 9) is a negative regulator of the hepatic LDL receptor, and clinical studies with PCSK9-inhibiting antibodies have demonstrated strong LDL-c-lowering effects. Here we screened phage-displayed peptide libraries and identified the 13-amino acid linear peptide Pep2-8
Yingnan Zhang et al.
Nature structural & molecular biology, 24(10), 848-856 (2017-08-22)
Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates plasma LDL cholesterol (LDL-c) levels by promoting the degradation of liver LDL receptors (LDLRs). Antibodies that inhibit PCSK9 binding to the EGF(A) domain of the LDLR are effective in lowering LDL-c. However, the

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