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

Alirocumab  (Synonyms: 阿利西尤单抗; REGN 727; SAR 236553)

目录号: HY-P9928 纯度: 97.00%
Data Sheet SDS COA 技术支持

Alirocumab 是一种抗 PCSK9 人单克隆抗体。Alirocumab 可抑制 PCSK9。Alirocumab 可减少 NLRP3 inflammasome,调节 Nrf2/HO-1HMGB1/NF-κBFractalkine/CX3CR1。Alirocumab 可增强肝脏结合 LDL 胆固醇 (LDL-C) 的能力,并降低血液中的 LDL-C 水平。Alirocumab 可改善动脉粥样硬化和炎症。

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CAS No. : 1245916-14-6

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

同型

Human IgG1 kappa

推荐同型对照抗体
种属

Human

体外研究
(In Vitro)

Alirocumab (40 μg/mL,24 h) 可减轻肥胖胰岛素抵抗 Zucker 大鼠 (OZR) 血管平滑肌细胞 (VSMC) 中基础 PCSK9 过表达[3]
Alirocumab (8 μg/mL,72 h) 通过抑制 PCSK9 减弱原代人肝细胞中的 Lp(a) 分泌[4]
Alirocumab (10 μg/mL,24 h) 可抑制 HepG2 细胞中脂质诱导的炎症[5]

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

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%.
体内研究
(In Vivo)

Alirocumab (3-10 mg/kg,皮下注射,18 周) 可抑制动脉粥样硬化、改善斑块形态并增强他汀类药物对 APOE*3Leiden.CETP 小鼠的作用[6]
Alirocumab (16 mg/kg/周,皮下注射,第 0 天、第 7 天和第 14 天) 可通过调节 Nrf2/HO-1、PCSK9/HMGB1/NF-ᴋB/NLRP3 和 Fractalkine/CX3CR1 枢纽来增强抗氧化状态阻止脓毒症诱发的肾毒性大鼠模型中的炎症[7]
Alirocumab (50 mg/kg,皮下注射,每周一次,在接触液体饮食之前) 减轻大鼠脑内乙醇诱导的神经元损伤和氧化应激[8]
Alirocumab (1 mg/kg/周,皮下注射) 激活棕色脂肪,增加肝脏对富含胆固醇的 TRL 残留物的摄取,从而降低非 HDL-C,并增加 HDL-C 水平和 HDL 胆固醇流出能力,进一步改善 APOE*3-Leiden.CETP 小鼠的血脂异常[9]
Alirocumab (10 mg/kg,皮下注射,2 周) 通过降低载脂蛋白 (a) 的产生率来降低非人类灵长类动物的脂蛋白 (a) 水平[10]
Alirocumab (3-10 mg/kg,腹腔注射,每周一次,持续 16 周) 可降低肥胖小鼠肺组织中的 RAS、NLRP3 炎症小体和胆囊收缩素[11]

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
NCT NumberSponsorConditionStart DatePhase
NCT01954394Sanofi|Regeneron Pharmaceuticals
Hypercholesterolemia
December 17, 2013Phase 3
NCT05469347Jonathan Sevransky|Regeneron Pharmaceuticals|Emory University
Sepsis
January 4, 2023Phase 1
NCT03004001Gloria Vega|Regeneron Pharmaceuticals|Aventis Pharmaceuticals|Dallas VA Medical Center
Nephrotic Syndrome
January 2017Phase 2
CAS 号
性状

液体

颜色

Colorless to light yellow

中文名称

阿利西尤单抗

储存方式

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

Format
  • Human IgG1 kappa
纯度 & 产品资料

纯度: 97.00%

参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 抗体抑制剂请问怎么灭菌呢?

    我们的抗体抑制剂产品本身就是无菌的,细胞实验可以用培养基稀释,动物实验可以用无菌 PBS 或者生理盐水稀释。

  • 抗体抑制剂的人源化,人鼠嵌合抗体有什么区别呢?

    人鼠嵌合抗体由鼠源可变区+人源恒定区组成,人源化约65%,免疫原性较高。人源化抗体仅保留鼠源CDR,其余为人源结构,人源化约90%,免疫原性较低。相比嵌合抗体,人源化抗体更接近人体抗体,安全性更高。

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