Alirocumab

Alirocumab is an anti-PCSK9 human monoclonal antibody. Alirocumab inhibits PCSK9. Alirocumab reduces NLRP3 inflammasome, regulates Nrf2/HO-1, HMGB1/NF-κB and Fractalkine/CX3CR1. Alirocumab increases the ability of the liver to bind LDL-cholesterol (LDL-C) and reduces levels of LDL-C in blood. Alirocumab improves atherosclerosis and inflammation[1][2][3][4][5][6][7][8][9][10][11].

Product Specifications

CAS Number

[1245916-14-6]

Product Name Alternative

REGN 727; SAR 236553

UNSPSC

12352203

Target

CX3CR1; HMG Family; Keap1-Nrf2; NF-κB; NOD-like Receptor (NLR) ; PCSK9

Type

Inhibitory Antibodies

Related Pathways

Cell Cycle/DNA Damage; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cardiovascular Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/alirocumab.html

Purity

97.00

Solubility

H2O

Smiles

OC(CO)COP(O)(O)=O.[Na].[Na]

Molecular Weight

(146.24 kDa)

References & Citations

[1]Markham A. Alirocumab: First Global Approval. Drugs. 2015;75 (14) :1699-1705. |[2]Tavori H, et al. Alirocumab: PCSK9 inhibitor for LDL cholesterol reduction. Expert Rev Cardiovasc Ther. 2014 Oct;12 (10) :1137-44.|[3]Barale C, et al. PCSK9 Expression in Vascular Smooth Muscle Cells: Role of Insulin Resistance and High Glucose. Int J Mol Sci. 2025 Jan 24;26 (3) :1003.|[4]Villard EF, et al. PCSK9 Modulates the Secretion But Not the Cellular Uptake of Lipoprotein (a) Ex Vivo: An Effect Blunted by Alirocumab. JACC Basic Transl Sci. 2016 Oct;1 (6) :419-427.|[5]Zhang X Y, et al. Conditional knockdown of hepatic PCSK9 ameliorates high-fat diet-induced liver inflammation in mice. Frontiers in Pharmacology, 2025, 16: 1528250.|[6]Kühnast S, et al. Alirocumab inhibits atherosclerosis, improves the plaque morphology, and enhances the effects of a statin. J Lipid Res. 2014 Oct;55 (10) :2103-12.|[7]Hassan NF, et al. Alirocumab boosts antioxidant status and halts inflammation in rat model of sepsis-induced nephrotoxicity via modulation of Nrf2/HO-1, PCSK9/HMGB1/NF-ᴋB/NLRP3 and Fractalkine/CX3CR1 hubs. Biomed Pharmacother. 2024 Aug;177:116929.|[8]Wagner J, et al. PCSK9 inhibition attenuates alcohol-associated neuronal oxidative stress and cellular injury. Brain Behav Immun. 2024 Jul;119:494-506.|[9]Zhou E, et al. Beneficial effects of brown fat activation on top of PCSK9 inhibition with alirocumab on dyslipidemia and atherosclerosis development in APOE*3-Leiden.CETP mice. Pharmacol Res. 2021 May;167:105524.|[10]Croyal M, et al. PCSK9 inhibition with alirocumab reduces lipoprotein (a) levels in nonhuman primates by lowering apolipoprotein (a) production rate. Clin Sci (Lond) . 2018 May 31;132 (10) :1075-1083. |[11]Liang L, et al. Statin administration or blocking PCSK9 alleviates airway hyperresponsiveness and lung fibrosis in high-fat diet-induced obese mice. Respir Res. 2024 May 18;25 (1) :213.