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
| Molecular Weight | 145981.36 |
| Formula | C6472H9996N1736O2032S42 |
| CAS Number | 1245916-14-6 |
| Storage | -80°C for long term |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PCSK9 Products |
|---|
| NNC0385-0434
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. |
| CiVi-007
CiVi-007 is an antisense oligonucleotide (ASO) polymerized with N-acetylglucosamine that targets PCSK9 and can be used in studies related to hypercholesterolemia. |
| AZD-8233
AZD-8233 is an orally active, antisense oligonucleotide (ASO) targeting PCSK9 that targets and inhibits the translation and protein synthesis of PCSK9 mRNA in hepatocytes and reduces circulating LDL-C levels. It can be used in studies related to hypercholesterolemia. |
| Ebronucimab
Ebronucimab is a monoclonal antibody to PCSK9 that can be used in studies related to hypercholesterolemia. |
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