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PCSK9-LDLR TR-FRET Assay Kit

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.Need us to run inhibitor screens or profile your compounds against PCSK9-LDLR? Check out ourPCSK9 Screening Services.This product has beencited 1 time.

Product Specifications

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

UniProt

Q8NBP7

Applications

Useful for screening small molecular inhibitors for drug discovery and HTS applications.

Format

Catalog #ComponentAmountStorage79079LDLR-Eu*2 µg-80°CAvoid freeze/ thaw cycles71304PCSK9, Biotinylated*35 µg-80°CDye-Labeled Acceptor2 x 10 µl-20°C332983x PL-01 Assay Buffer4 ml-20°C79969White, Nonbinding, low volume, 384-well microtiter plate1Room Temp*The concentration of LDLR-Eu and PCSK9 are lot-specific and will be indicated on the tubes containing the protein

Shipping Conditions

-80°C

Storage Conditions

At least 6 months from date of receipt when stored as directed.

Frequently Asked Questions

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