PCSK9-IN-30

• UNSPSC Description:

  PCSK9-IN-30 (Compound 3f) is a PCSK9 inhibitor. PCSK9-IN-30 interacts with a cryptic binding groove of PCSK9, inhibiting the binding of PCSK9 to the low-density lipoprotein receptor (LDLR) (IC50 = 537 nM), restoring the uptake of low-density lipoprotein (LDL) by liver cells, and ultimately reducing plasma cholesterol levels. PCSK9-IN-30 exhibits good bioavailability in mice and can be used for research in the field of cardiovascular diseases[1].

• Target Antigen:

  PCSK9

• Type:

  Reference compound

• Related Pathways:

  Metabolic Enzyme/Protease

• Field of Research:

  Cardiovascular Disease

• Assay Protocol:

  https://www.medchemexpress.com/pcsk9-in-30.html

• Smiles:

  CC1=CN(C=N1)C2=CC(NC(C3=CC(OC4=CC=CC=C4)=C(C)C=C3)=O)=CC(CN5C[C@H](N)CCC5)=C2

• Molecular Weight:

  495.62

• References & Citations:

  [1]Bao X, et al. Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside. Signal Transduct Target Ther. 2024 Jan 8;9(1):13.|[2]Evison BJ, et al. A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove. Bioorg Med Chem. 2020 Mar 15;28(6):115344.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported