Dim16
Dim16 is a dual PCSK9 inhibitor and HMG-CoAR inhibitor, with an IC50 of 0.8 nM against human PCSK9 and an IC50 of 146.8 μM against HMG-CoAR. Dim16 disrupts the PCSK9-LDLR protein-protein interaction, inhibits the catalytic activity of HMG-CoAR, enhances cellular uptake of extracellular LDL, and suppresses PCSK9-induced platelet aggregation. Dim16 can be used in research related to hypercholesterolemia.
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- CAS. Nr.: 2743448-32-8
- Formel: C29H38IN5
- Molecular Weight:583.55
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
19 nM (PCSK9)[1]
Dim16 (0.1-1×106 nM; 2 h) potently inhibits the protein-protein interaction between PCSK9 and LDLR in a biochemical assay with an IC50 of 0.8 nM[1].
Dim16 (10-500 μM; 10 min) inhibits HMG-CoAR activity in a biochemical assay with an IC50 of 146.8 μM[1].
Dim16 (0.1 nM-10000 nM; 48 h) is non-toxic to HepG2 cells[1].
Dim16 (1-10 nM; 2 h) restores cell surface LDLR levels in PCSK9-treated HepG2 cells[1].
Dim16 (1-10 nM; 2 h co-incubation with PCSK9, 2 h incubation with fluorescent LDL) restores and enhances LDL uptake in PCSK9-treated HepG2 cells[1].
Dim16 (10 nM; 15 min preincubation with PCSK9) prevents the PCSK9-induced potentiation of epinephrine-stimulated platelet aggregation in human platelet-rich plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
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Incubation Time:48 h
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Result:Showed no reduction in HepG2 cell vitality at any tested concentration compared to control cells.
Chemical Information
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CAS. Nr. 2743448-32-8
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Molecular Weight 583.55
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Formel C29H38IN5
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SMILES
CC(C)(C)CCCN1C(C2=CN=C(N2CCCCCNC)I)=NC=C1C3=CC=C4C=CC=CC4=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Dim16 Related Classifications
HY-149310 Related Classifications
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