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.
| Molecular Weight | 141788.63 |
| Formula | C6242H9648N1668O1996S56 |
| CAS Number | 1256937-27-5 |
| 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.
[3] Weinreich M, et al. Cardiol Rev. Antihyperlipidemic therapies targeting PCSK9.
| 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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