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Evolocumab is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). Evolocumab binds to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface. PCSK9 is a protein that targets LDL receptors for degradation and thereby reduces the liver's ability to remove LDL-C, or "bad" cholesterol, from the blood. In the absence of PCSK9, there are more LDL receptors on the surface of liver cells to remove LDL-C from the blood. Evolocumab has antioxidant and cytoprotective activities against H2O2-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation.
| Molecular Weight | 141788.63 |
| Formula | C6242H9648N1668O1996S56 |
| CAS Number | 1256937-27-5 |
| Storage | -80°C for long term |
[3] Weinreich M, et al. Cardiol Rev. Antihyperlipidemic therapies targeting PCSK9.
| Related PCSK9 Products |
|---|
| PCSK9-IN-13
PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM. |
| PCSK9 ligand 1
PCSK9 ligand 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) ligand. |
| AZD0780
AZD0780 (PCSK9-IN-12, EX-A6975) is an oral, potentially first-in-class small molecule inhibitor of PCSK9. AZD0780 (PCSK9-IN-12, EX-A6975) has bind affinity for PCSK9 with a Kd value of ＜200 nM. AZD0780 (PCSK9-IN-12, EX-A6975) can be used for the research of cholesterol metabolism. |
| NNC0385-0434
NNC0385-0434 is a peptide based on the epidermal growth-factor-like domain A of the human LDLR peptide. NNC0385-0434 competitively binds free PCSK9 and subsequently prevents PCSK9 binding to the LDLR. NNC0385-0434 is an orally active peptide small molecule PCSK9 inhibitor for atherosclerosis-related studies. |
| CiVi-008
CiVi-008 is an orally active PCSK9 antisense oligonucleotide (ASO) inhibitor for studies related to disorders of lipid metabolism. |
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