5.08761

PCSK9 Inhibitor, EGF-A

• Synonyme(s) : PCSK9 Inhibitor, EGF-A
• Formule empirique (notation de Hill): C₁₈₈H₂₉₂N₅₈O₆₅S₆
• Poids moléculaire : 4597.07
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Essai: ≥95% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 0.3 μM K_i
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: white
• Solubilité: water: 25 mg/mL
• Température de stockage: −20°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Primary Target
PCSK9

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Séquence

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

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable