Dim16 hydrochloride
Dim16 hydrochloride 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 hydrochloride 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 hydrochloride can be used in research related to hypercholesterolemia.
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- No. CAS: 2743448-41-9
- Fòrmula: C29H39ClIN5
- Peso molecular:620.01
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Descripciòn
In Vitro
Dim16 (0.1-1×106 nM; 2 h) hydrochloride 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) hydrochloride inhibits HMG-CoAR activity in a biochemical assay with an IC50 of 146.8 μM[1].
Dim16 (0.1 nM-10000 nM; 48 h) hydrochloride is non-toxic to HepG2 cells[1].
Dim16 (1-10 nM; 2 h) hydrochloride 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) hydrochloride restores and enhances LDL uptake in PCSK9-treated HepG2 cells[1].
Dim16 (10 nM; 15 min preincubation with PCSK9) hydrochloride 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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No. CAS 2743448-41-9
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Peso molecular 620.01
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Fòrmula C29H39ClIN5
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SMILES
IC1=NC=C(N1CCCCCNC)C2=NC=C(N2CCCC(C)(C)C)C3=CC4=C(C=CC=C4)C=C3.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dim16 hydrochloride Related Classifications
HY-149310A Related Classifications
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