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Alirocumab (anti-PCSK9)

MCE China：Alirocumab (anti-PCSK9)

Brand：MedChemExpress (MCE)

Cat. No.HY-P9928A

CAS：1245916-14-6

Synonyms：REGN 727(anti-PCSK9); SAR 236553(anti-PCSK9)

Purity：98.24%

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Shipping with dry ice.

Description：Alirocumab (anti-PCSK9) is an anti-PCSK9 human monoclonal antibody. Alirocumab (anti-PCSK9) inhibits PCSK9. Alirocumab (anti-PCSK9) reduces NLRP3 inflammasome, regulates Nrf2/HO-1, HMGB1/NF-κB and Fractalkine/CX3CR1. Alirocumab (anti-PCSK9) increases the ability of the liver to bind LDL-cholesterol (LDL-C) and reduces levels of LDL-C in blood. Alirocumab (anti-PCSK9) improves atherosclerosis and inflammation.

In Vitro：Alirocumab (anti-PCSK9) (40 μg/mL, 24 h) alleviates basal PCSK9 overexpression in vascular smooth muscle cells (VSMCs) of obese insulin-resistant Zucker rats (OZR)[3]. Alirocumab (anti-PCSK9) (8 μg/mL, 72 h) attenuates Lp(a) secretion in primary human hepatocytes via inhibition of PCSK9[4]. Alirocumab (anti-PCSK9) (10 μg/mL, 24 h) inhibits lipid-induced inflammation in HepG2 cells[5].

In Vivo：Alirocumab (anti-PCSK9) (3-10 mg/kg, s.c., 18 weeks) inhibits atherosclerosis, improves the plaque morphology, and enhances the effects of a statin in APOE*3Leiden.CETP mice[6]. Alirocumab (anti-PCSK9) (16 mg/kg/week, s.c., on day 0, day 7, and day 14) 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[7]. Alirocumab (anti-PCSK9) (50 mg/kg, s.c., weekly prior to exposure to the liquid diets) attenuates ethanol-induced neuronal injury in the brain and oxidative stress in rats s[8]. Alirocumab (anti-PCSK9) (1 mg/kg/week, s.c.) activates brown fat, increases hepatic uptake of cholesterol-rich TRL remnants, thereby lowering non-HDL-C, and increases HDL-C levels and cholesterol efflux capacity of HDL, further improving dyslipidemia in APOE*3-Leiden.CETP mice[9]. Alirocumab (anti-PCSK9) (10 mg/kg, s.c., 2 weeks) reduces lipoprotein(a) levels in nonhuman primates by lowering apolipoprotein(a) production rate[10]. Alirocumab (anti-PCSK9) (3-10 mg/kg, i.p., weekly for 16 weeks) reduces RAS, NLRP3 inflammasome, and cholecystokinin in lung tissue of obese mice[11].

IC50 & Target：HMGB

Species：Human

Isotype：Human IgG1 kappa

Recommend Isotype Controls：Human IgG1 kappa, Isotype Control

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References：

[1]. Markham A. Alirocumab: First Global Approval. Drugs. 2015;75(14):1699-1705.  [Content Brief]

[2]. Tavori H, et al. Alirocumab: PCSK9 inhibitor for LDL cholesterol reduction. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1137-44.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[8]. Wagner J, et al. PCSK9 inhibition attenuates alcohol-associated neuronal oxidative stress and cellular injury. Brain Behav Immun. 2024 Jul;119:494-506.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]