All AbMole products are for research use only, cannot be used for human consumption.
Alirocumab works by inhibiting the PCSK9 protein. PCSK9 binds to the low-density lipoprotein receptor (LDLR) (which takes cholesterol out of circulation), and that binding leads to the receptor being degraded, and less LDL cholesterol being removed from circulation. Inhibiting PCSK9 prevents the receptor from being degraded, and promotes removal of LDL cholesterol from circulation. After subcutaneous administration of alirocumab, maximal suppression of free PCSK9 occurs within 4 to 8 hours and has an apparent half-life of 17 to 20 days. Inhibition is dose-dependent. The antibody is distributed through the circulation, and it is eliminated at low concentrations by binding to its target, and at higher concentrations through a proteolytic pathway.
Metabolism. 2024 Jan;6:152:155774.
Inhibition of PCSK9 prevents and alleviates cholesterol gallstones through PPARα-mediated CYP7A1 activation
Alirocumab purchased from AbMole
Circulation. 2023 May 26.
Immune Regulation of the Liver Through the PCSK9/CD36 Pathway During Heart Transplant Rejection
Alirocumab purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | PSC-CMs, hPSC-ECs, H9C2, HUVECs |
| Preparation method | Human PSC-CMs between day 30 andday 40 or hPSC-ECs between day 10 and day 20, as well as the cardiomyocyte line H9C2 and human umbilical vein endothelial cells (HUVECs), were used for cell viability assays. The analyses were performed 24, 48, or 72 h after drug exposure. The concentrations of alirocumab were set at 0.01, 0.1, 1, 2, and 10 μM (that is 0.1, 1, 10, 20, and 100 times the peak serum concentration of 15 μg/mL), while the concentrations of atorvastatin were set at 0.05, 0.5, 5, 10, and 50 μM (0.1, 1, 10, 20, and 100 times the peak serum concentration of 252 ng/mL) |
| Concentrations | 0.01, 0.1, 1, 2, and 10 μM |
| Incubation time | 24, 48, or 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague–Dawley rats |
| Formulation | Saline |
| Dosages | 10 mg/kg |
| Administration | Intraperitoneal injection |
| Molecular Weight | 145981.36 |
| Formula | C6472H9996N1736O2032S42 |
| CAS Number | 1245916-14-6 |
| Storage | -80°C for long term |
| Related PCSK9 Products |
|---|
| Pep2-8
Pep2-8 is a PCSK9 inhibitor, of which KD The value is 0.7 μM,IC50 The value is 1.4 μM. |
| Evolocumab
Evolocumab (AMG 145) is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. |
| 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. |
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