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PCSK9 ligand 1 

Cat. No.: HY-130245
Handling Instructions

PCSK9 ligand 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM.

For research use only. We do not sell to patients.

PCSK9 ligand 1 Chemical Structure

PCSK9 ligand 1 Chemical Structure

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Description

PCSK9 ligand 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM[1].

IC50 & Target

Ki: 107 nM (PCSK9)[1]

In Vitro

PCSK9 ligand 1 ( Compound 16; 1.25-20 μM; 24 hours; HEK293 cells) treatment shows a clear concentration-dependent degradation of both the pro and mature form of PCSK9 yielding a half-maximal degradation concentration of 4.8 and 3.4 μM, as well as a maximum percentage of degradation at 20 μM of 58% and 61%, respectively[1].

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 1.25 μM, 2.5 μM, 5 μM, 10 μM or 20 μM
Incubation Time: 24 hours
Result: Showed a clear concentration-dependent degradation of both the pro and mature form of PCSK9 yielding a half-maximal degradation concentration of 4.8 and 3.4 μM, as well as a maximum percentage of degradation at 20 μM of 58% and 61%, respectively.
Molecular Weight

1077.22

Formula

C₅₃H₆₉FN₈O₁₃S

SMILES

OC(C(C=C1)=CC=C1C(C(F)=C2)=CC=C2OC(C(OCCOCCNC([[email protected]@H](NC(OC(C)(C)C)=O)CCCN/C(NC(OC(C)(C)C)=O)=N/C(OC(C)(C)C)=O)=O)=C3)=CC4=C3CCN[[email protected]]4(C)CC(NC5=NC=CS5)=O)=O

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Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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PCSK9 ligand 1
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HY-130245
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