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Product Details
FAB
- Comprehensive validation - Validated with various antibody and peptide drugs.
- Simple and fast operation - No complicated washing steps, significantly reducing time.
- High batch consistency - Strict control over raw materials and finished product quality, ensuring a stable supply.
- Accurate and reliable results - High sensitivity with minimal matrix effects.
- High throughput capability - Support multiple product specifications, ideal for high-throughput screening.
- Fast completion - Results in just 1 hour.
Product Specifications
Assay TypeCompetition-TR-FRETReactivityHumanRegulatory StatusRUOAssay Time1 hrSample volume5 μLProduct Overview
The Human PCSK9 / LDL R Inhibitor Screening Kit (TR-FRET) is based on a homogeneous (no wash) competition TR-FRET technology (Time-Resolved Fluorescence Resonance Energy Transfer) to screen for inhibitors of human PCSK9 binding to LDL R within one hour. It can also be used as a universal detection tool to identify the ability of human PCSK9 to bind to human LDL R.
Storage
1. Store the unopened kit at 2-8°C upon receipt.
2. Locate the expiration date on the outer packaging and do not use reagents beyond their expiration date.
3. The opened kit should be stored according to the storage conditions listed in the Components Table. The shelf life of the opened kit is 30 days from the date of opening.
Materials Provided
IDComponentsSizeFRTP040-C01Human PCSK9 Protein Europium-chelate100 tests/500 testsFRTP040-C02FA-Labeled Human LDL R Protein100 tests/500 testsFRTP040-C03Anti-PCSK9 Neutralizing Antibody30 μg/100 tests
150 μg/500 testsFRTP040-C04Signal Enhancer8 mL/100 tests & 500 testsDB-04TR-FRET Sample Dilution Buffer, pH7.450 mL/100 tests & 500 testsDB-07TR-FRET Detection Buffer, for pH5.5 reaction system50 mL/100 tests & 500 testsAssay Principles
This Human PCSK9 / LDL R Inhibitor Screening Kit (TR-FRET) is based on TR-FRET technology (Time-Resolved Fluorescence Resonance Energy Transfer). This assay uses the mixture of biotinylated human PCSK9 and Europium-chelate labeled streptavidin as the Donor and FA-Labeled Human LDL R Protein as the Acceptor.
— When the sample does not contain the inhibitors that block the binding of human PCSK9 to human LDL R, the Donor and Acceptor are in close proximity because of the binding of human PCSK9 and human LDL R. Upon Donor excitation with light of a specific wavelength (337 nm), in addition to Donor emission (620 nm), non-radiative transfer of energy occurs between Donor and Acceptor, resulting in Acceptor emission (665 nm).
— When the sample contains the inhibitors that block the binding of human PCSK9 to human LDL R, the components inhibit the binding between the Donor and Acceptor and thereby prevent FRET from occurring.
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Performance Data
Bioactivity-TR-FRET
Please refer to DS document for the assay protocol.
In this TR-FRET assay, Human PCSK9 Protein Europium-chelate is used as the Donor and FA-Labeled Human LDL R Protein is used as the Acceptor. An inhibition Assay was performed to evaluate the interaction between human PCSK9 and human LDL R using Anti-PCSK9 Antibody resulting in a typical IC50 of 1.653 nM (QC tested).
The kit is suitable for the detection and characterization of PCSK9 / LDL R inhibitors. It was shown that the anti-PCSK9 antibody (Recaticimab) disrupted the interaction, with an IC50 of 1.614 nM. The anti-TNF-alpha antibody (Adalimumab) showed no significant inhibitory effect in the assay as expected.
The kit is suitable for the detection and characterization of PCSK9 / LDL R inhibitors such as peptide drugs. It was shown that the Enlicitide chloride disrupted the interaction, with an IC50 of 37.13 nM.
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Drug Development Progress- English Name：
Proprotein convertase subtilisin kexin type 9
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Approved
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