PCSK9-LDLR TR-FRET Assay Kit

Catalog #
72010
$905 *
Size: 384 reactions
Qty
*US Pricing only. For international pricing, please contact your local distributor.
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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.

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This product has been cited 1 time.

Synonyms
pcsk9, cholesterol, LDL, kexin
Product Info
Storage and Usage
Citations1
Assay Kit Format
TR-FRET
Supplied As
Kit comes in a convenient format with biotinylated PCSK9, Eu-labeled LDLR, dye-labeled acceptor, assay buffer and microtiter plate to perform 384 reactions.
Materials Required But Not Supplied

Fluorescent microplate reader capable of measuring Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET)
Adjustable micropipettor and sterile tips

Format
Catalog # Component Amount Storage
79079 LDLR-Eu* 2 µg -80°C Avoid freeze/ thaw cycles
71304 PCSK9, Biotinylated*  35 µg -80°C
  Dye-Labeled Acceptor 2 x 10 µl -20°C
33298 3x PL-01 Assay Buffer 4 ml -20°C
79969 White, Nonbinding, low volume, 384-well microtiter plate 1 Room Temp

*The concentration of LDLR-Eu and PCSK9 are lot-specific and will be indicated on the tubes containing the protein  

UniProt #
Q8NBP7
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
References

1. Chan, J.C. et al. (2009). Proc. Natl Acad. Sci. USA, 106, 9820-9825.
2. Liang, H., et al. (2012) J. Pharmacol. Exp. Ther. 340 2289-236.