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  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: 阿利西尤單抗; REGN 727; SAR 236553)

目錄號(hào): HY-P9928 純度: 97.00%
COA 技術(shù)支持

Alirocumab 是一種抗 PCSK9 人單克隆抗體。Alirocumab 可抑制 PCSK9。Alirocumab 可減少 NLRP3 inflammasome，調(diào)節(jié) Nrf2/HO-1、HMGB1/NF-κB 和 Fractalkine/CX3CR1。Alirocumab 可增強(qiáng)肝臟結(jié)合 LDL 膽固醇 (LDL-C) 的能力，并降低血液中的 LDL-C 水平。Alirocumab 可改善動(dòng)脈粥樣硬化和炎癥。

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CAS No. : 1245916-14-6

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5 mg ￥9400
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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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
推薦同型對(duì)照抗體
種屬

Human
體外研究
(In Vitro)

Alirocumab (40 μg/mL，24 h) 可減輕肥胖胰島素抵抗 Zucker 大鼠 (OZR) 血管平滑肌細(xì)胞 (VSMC) 中基礎(chǔ) PCSK9 過(guò)表達(dá)[3]。
Alirocumab (8 μg/mL，72 h) 通過(guò)抑制 PCSK9 減弱原代人肝細(xì)胞中的 Lp(a) 分泌[4]。
Alirocumab (10 μg/mL，24 h) 可抑制 HepG2 細(xì)胞中脂質(zhì)誘導(dǎo)的炎癥[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%.
體內(nèi)研究
(In Vivo)

Alirocumab (3-10 mg/kg，皮下注射，18 周) 可抑制動(dòng)脈粥樣硬化、改善斑塊形態(tài)并增強(qiáng)他汀類藥物對(duì) 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) 可通過(guò)調(diào)節(jié) Nrf2/HO-1、PCSK9/HMGB1/NF-?B/NLRP3 和 Fractalkine/CX3CR1 樞紐來(lái)增強(qiáng)抗氧化狀態(tài)阻止膿毒癥誘發(fā)的腎毒性大鼠模型中的炎癥[7]。
Alirocumab (50 mg/kg，皮下注射，每周一次，在接觸液體飲食之前) 減輕大鼠腦內(nèi)乙醇誘導(dǎo)的神經(jīng)元損傷和氧化應(yīng)激[8]。
Alirocumab (1 mg/kg/周，皮下注射) 激活棕色脂肪，增加肝臟對(duì)富含膽固醇的 TRL 殘留物的攝取，從而降低非 HDL-C，并增加 HDL-C 水平和 HDL 膽固醇流出能力，進(jìn)一步改善 APOE*3-Leiden.CETP 小鼠的血脂異常[9]。
Alirocumab (10 mg/kg，皮下注射，2 周) 通過(guò)降低載脂蛋白 (a) 的產(chǎn)生率來(lái)降低非人類靈長(zhǎng)類動(dòng)物的脂蛋白 (a) 水平[10]。
Alirocumab (3-10 mg/kg，腹腔注射，每周一次，持續(xù) 16 周) 可降低肥胖小鼠肺組織中的 RAS、NLRP3 炎癥小體和膽囊收縮素[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-?B 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 號(hào)
性狀

液體

顏色

Colorless to light yellow

中文名稱

阿利西尤單抗
儲(chǔ)存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
Format
  • Human IgG1 kappa
純度 & 產(chǎn)品資料

純度: 97.00%

參考文獻(xiàn)

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  • 稀釋計(jì)算器

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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.

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產(chǎn)品名稱：
Alirocumab
目錄號(hào)：
HY-P9928
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