5.08761

PCSK9 Inhibitor, EGF-A

• 别名: PCSK9 Inhibitor, EGF-A
• 经验公式（希尔记法）: C₁₈₈H₂₉₂N₅₈O₆₅S₆
• 分子量: 4597.07
• UNSPSC代码: 12352200
• NACRES: NA.77

属性

• 方案: ≥95% (HPLC)
• 质量水平: 100
• 表单: powder
• 效能: 0.3 μM K_i
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; desiccated (hygroscopic); protect from light
• 颜色: white
• 溶解性: water: 25 mg/mL
• 储存温度: −20°C

说明

一般描述

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.

生化/生理作用

Primary Target
PCSK9

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

序列

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

重悬

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

其他说明

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

法律信息

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

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable