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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 |
[2] Weinreich M, et al. Cardiol Rev. Antihyperlipidemic therapies targeting PCSK9.
| Related PCSK9 Products |
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| Alirocumab
Alirocumab is a humanized IgG1 PCSK9 monoclonal antibody that can be used in the study of hypercholesterolemia. |
| Schizandrol-B
Schisantherin B (Gomisin-B; Wuweizi ester-B; Schisantherin-B) is a lignan from Schisandra chinensis that promotes liver enlargement in mice through activation of the PXR and YAP pathways and inhibits PCSK9 protein expression with an IC50 value of 1.10 μM. |
| R-IMPP
R-impp (PF-00932239) is an anti-secreting inhibitor of PCSK9 (IC50=4.8 μM), which can inhibit PCSK9 protein translation by targeting the ribosomes at the time of 80S. |
| SBC-115076
Sbc-115076 is an effective inhibitor of the preprotein invertase Bacillus subtilis proteinase/Kexin 9 (PCSK9). PCSK9 is a preprotein invertase that plays an important role in LDL receptor metabolism. |
| SBC-110736
SBC-110736 is a novel inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9). |
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