2. Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Cell Cycle/DNA Damage
  3. PCSK9 NOD-like Receptor (NLR) Keap1-Nrf2 HMG Family NF-κB CX3CR1
  4. Alirocumab

Alirocumab  (Synonyms: REGN 727; SAR 236553)

Cat. No.: HY-P9928 Purity: 97.00%
SDS COA Technical Support

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.

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CAS No. : 1245916-14-6

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Alirocumab Related Antibodies

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Description

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].

Isotype

Human IgG1 kappa
Recommend Isotype Controls
Species

Human
In Vitro

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Alirocumab Related Antibodies

Western Blot Analysis[5]

Cell Line: HepG2 incubated with 0.5 mM cis-9-octadecenoic acid and 0.25 mM palmitic acid
Concentration: 10 μg/mL
Incubation Time: 24 h
Result: Decreased PCSK9 protein levels by 65.3%.
Attenuated increased IL-6, IL-1β, and TNFα protein levels.
Decreased p65-NF-κB phosphorylation.
Reduced the phosphorylation levels of AP-1 by 61.0%.
Decreased the phosphorylation levels of PI3K and AKT.
Decreased the mTOR protein phosphorylation levels by 46.2%.
In Vivo

Alirocumab (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 (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 (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[8].
Alirocumab (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 (10 mg/kg, s.c., 2 weeks) reduces lipoprotein(a) levels in nonhuman primates by lowering apolipoprotein(a) production rate[10].
Alirocumab (3-10 mg/kg, i.p., weekly for 16 weeks) reduces RAS, NLRP3 inflammasome, and cholecystokinin in lung tissue of obese mice[11].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male albino Wistar rats model (LPS-intoxicated)[7]
Dosage: 16 mg/kg/week
Administration: Subcutaneous injection (s.c.), on day 0, day 7, and day 14
Result: Mitigated LPS-mediated increments in serum creatinine and cystatin C, together with renal contents of both KIM-1 and NGAL.
Restored renal NGAL content to its normal values.
Boosted mRNA expression levels of both Nrf2 and HO-1 and renal TAC content (2.5, 2, and 3.2-folds, respectively).
Produced pronounced hampering in LPS-mediated elevation in mRNA expression levels of PCSK9 and RAGE, along with renal contents of PCSK9 and HMGB1 by 80.9 %, 49.6 %, 53.1 % and 59.8 %, respectively.
Resulted in a marked reduction in the protein expression of TLR4, MYD88, and NLRP3, along with mRNA expression levels of NF-ᴋB by 62.9 %, 58.1 %, 50.9 %, respectively.
Caused remarkable alleviation in LPS-mediated increment in TNF-α, IL-1β, and caspase-1 by 48.5 %, 68.3 % and 58.5 %, respectively.
Produced prominent downregulation in mRNA expression levels of CX3CL1 and CX3CR1 by 88.4 % and 87.5 %, respectively.
Exhibited prominent elevation in mRNA expression level of Bcl-2 (1.7-folds), along with a marked reduction in both mRNA expression level of Bax and renal caspase-3 content (by 66.7 % and 58.5 %, respectively) .
Regressed glomerular and tubular lesions.
Clinical Trial
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

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

Please store the product under the recommended conditions in the Certificate of Analysis.
Format
  • Human IgG1 kappa
Purity & Documentation

Purity: 97.00%

SDS (251 KB)

COA (231 KB)

Inhibitory Antibodies User Guide (602 KB)
References
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Alirocumab Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alirocumab1245916-14-6REGN 727 SAR 236553REGN727REGN-727SAR236553SAR 236553SAR-236553PCSK9NOD-like Receptor (NLR)Keap1-Nrf2HMG FamilyNF-κBCX3CR1Proprotein convertase subtilisin/kexin type 9High Mobility Group FamilyNuclear factor-κBNuclear factor-kappaBCX3C chemokine receptor1GPR13fractalkine receptorLDLhypercholesterolemiaInhibitorinhibitorinhibit

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