PCSK9-LDLR TR-FRET Assay Kit

Catalog #: 72010
Size: 384 reactions
$725
Background:
PCSK9 is a crucial player in the regulation of plasma cholesterol homeostasis. It binds to the ectodomain of hepatic low-density lipid receptor family members: low density lipoprotein receptor (LDLR), very low density lipoprotein receptor (VLDLR), apolipoprotein E receptor (LRP1/APOER) and apolipoprotein receptor 2 (LRP8/APOER2), and promotes their degradation. PCSK9 acts via a non-proteolytic mechanism to enhance the degradation of the hepatic LDLR through a clathrin LDLRAP1/ARH-mediated pathway. May prevent the recycling of LDLR from endosomes to the cell surface or direct it to lysosomes for degradation
Description:
The PCSK9/LDLR TR-FRET Assay Kit is designed to measure the inhibition of PCSK9 binding to LDLR in a homogeneous 384 reaction format. This FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; a sample containing europium-labeled (Eu) LDLR ectodomain, dye-labeled acceptor, biotin-labeled PCSK9, and an inhibitor is incubated for two hours. Then, the fluorescence intensity is measured using a fluorescence reader.
UniProt
Q8NBP7
Synonym(s):
pcsk9, cholesterol, LDL, kexin
Supplied As:
Kit comes in a convenient format with purified ATAD2A, ligands, Tb donor, dye-labeled acceptor, assay buffer and microtiter plate to perform 384 reactions.
Format:

COMPONENTS:

Instructions for use:
See assay kit data sheet for detailed protocol.
Storage / Stability:
At least 6 months from date of receipt when stored as directed.
Application(s):
Great for screening small molecular inhibitors for drug discovery and HTS applications.
Notes:
MATERIALS OR INSTRUMENTS REQUIRED BUT NOT SUPPLIED:
Fluorescent microplate reader capable of measuring Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET)
Adjustable micropipettor and sterile tips

Warning(s):
Avoid freeze/thaw cycles.
Scientific Category:
Cholesterol Related
Product Type:
Assay Kit
Data shown is lot-specific. Contact us for specific information on other lots.

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Product Datasheets

72010.pdf