Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular disease.

PCSK9-LDLR binding:2.08 ± 1.21 nM, PCSK9 (wt):1.94 ± 0.32 nM

METHODS: HUVECs were seeded in 96-well plates at a rate of 1 × 10*5 cells/well in logarithmic growth phase and treated with evolocumab in the concentration range of 0.5-100 mg/ml or vitamin C (Vit C; 50 and 100 mg /ml), then add new medium, expose HUVECs to 0.5 mM H2O2 for 2 hours, and detect HUVECs cell viability by MTT method.
RESULTS Evolocumab significantly inhibited H2O2-induced cytotoxicity at concentrations of 5-100 mg/ml. [2]
METHODS: Rat retinal Müller cells (RMCs) were used as the research object and treated with Evolocumab (100 μg/ml) to study the expression of inflammatory factors in RMCs.
RESULTS Evolocumab treatment (100 μg/ml) reduced the expression and secretion of inflammatory factors in stimulated RMCs (P<0.05), downregulated toll-like receptor-4 (TLR-4) levels in RMCs and inhibited nuclear transcription factor-κB ( NF-κB) phosphorylation (P < 0.05).[4]

METHODS: In a randomized placebo-controlled clinical study, evolocumab was administered at a dose of 140 mg/2 weeks (Q2W) or 420 mg once a month (QM) for 12 weeks, and LDL-C levels in the body were observed compared with placebo.
RESULTS On average, LDL-C was reduced by approximately 55%-75% at weeks 10 and 12 compared to placebo. [1]

Human

Immobilized Human PCSK9 Protein (His) (TMPY-00895) at 1 μg/mL (100 μL/well) can bind Evolocumab. The EC50 is 310.100 ng/mL.

Monoclonal

Unconjugated