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^[1].

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.

583.55

C₂₉H₃₈IN₅

2743448-32-8

CC(C)(C)CCCN1C(C2=CN=C(N2CCCCCNC)I)=NC=C1C3=CC=C4C=CC=CC4=C3

Room temperature in continental US; may vary elsewhere.

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

• [1]. Lammi C, et al. Computational Design, Synthesis, and Biological Evaluation of Diimidazole Analogues Endowed with Dual PCSK9/HMG-CoAR-Inhibiting Activity. J Med Chem. 2023 Jun 22;66(12):7943-7958.  [Content Brief]