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^[1].

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.

620.01

C₂₉H₃₉ClIN₅

2743448-41-9

IC1=NC=C(N1CCCCCNC)C2=NC=C(N2CCCC(C)(C)C)C3=CC4=C(C=CC=C4)C=C3.Cl

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;66(12):7943-7958.  [Content Brief]