1. Metabolic Enzyme/Protease Epigenetics Apoptosis Immunology/Inflammation Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  2. PCSK9 Small Interfering RNA (siRNA) Pyroptosis PPAR NOD-like Receptor (NLR) Caspase Interleukin Related
  3. Inclisiran

Inclisiran  (Synonyms: 英克司兰; ALN-PCSsc)

目录号: HY-132591 纯度: 99.80%
COA 产品使用指南 技术支持

Inclisiran 是一种双链小干扰 RNA (siRNA) 分子。Inclisiran 可抑制 PCSK9 的转录。Inclisiran 抑制焦亡 (Pyroptosis)、激活 PPARγ,减少 NLRP3cleaved caspase-1IL-1βIL-18。Inclisiran 具有抗炎、调节血脂、抗动脉粥样硬化活性。Inclisiran 可用于高脂血症和心血管疾病 (CVD) 研究。

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RNA, (Am-sp-(2'-deoxy-2'-fluoro)C-sp-Am-(2'-deoxy-2'-fluoro)A-(2'-deoxy-2'- fluoro)A-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)C-Am-(2'-deoxy-2'-fluoro)AAm-(2'-deoxy-2'-fluoro)A-Cm-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)G-Um-(2'-deoxy-2'-fluoro)C-Um-Am-Gm-sp-Am-sp-Am), complex with RNA (Cm-sp-Umsp -Am-Gm-Am-Cm-(2'-deoxy-2'-fluoro)C-Um-(2'-deoxy-2'-fluoro)G-Um-dT-UmUm-Gm-Cm-Um-Um-Um-Um-Gm-Um) 3'-[[(2S,4R)-1-[29-[[2-(acetylamino)-2- deoxy-β-D-galactopyranosyl]oxy]-14,14-bis[[3-[[3-[[5-[[2-(acetylamino)-2-deoxy-βD-galactopyranosyl]oxy]-1-oxopentyl]amino]propyl]amino]-3-oxopropoxy]methyl]- 1,12,19,25-tetraoxo-16-oxa-13,20,24-triazanonacos-1-yl]-4-hydroxy-2- pyrrolidinyl]methyl hydrogen phosphate] (1:1)

Inclisiran Chemical Structure

CAS No. : 1639324-58-5

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Customer Review

Other Forms of Inclisiran:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Inclisiran is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran inhibits the transcription of PCSK9. Inclisiran inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran can be used in researches of hyperlipidemia and cardiovascular disease (CVD)[1][2][3].

IC50 & Target[1][2][3]

PPARγ

 

IL-1β

 

Caspase-1

 

NLRP3

 

体外研究
(In Vitro)

Inclisiran (50-200 nM;48 h) 可显著抑制 ox-LDL 诱导的 HUVEC 中的细胞死亡和细胞毒性,并下调细胞焦亡相关因子的 mRNA 和蛋白质表达[2]
Inclisiran (50-200 nM;48 h) 可通过激活 PPARγ 通路抑制 Raw264.7 巨噬细胞中 ox-LDL 诱导的泡沫细胞形成[3]

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

Western Blot Analysis[2]

Cell Line: Human umbilical vein endothelial cells (HUVECs) treated with 25 μg/mL ox-LDL
Concentration: 50 nM, 100 nM, 200 nM
Incubation Time: 48 h
Result: Decreased the protein expression of NLRP3, ASC, cleaved caspase-1, GSDMD-N, IL-1β, and IL-18.

Western Blot Analysis[3]

Cell Line: Raw264.7 macrophages treated with ox-LDL
Concentration: 50 nM, 100 nM, 200 nM
Incubation Time: 48 h
Result: Increased PPARγ, SR-B1, ApoE, ABCA1.
Decreased SR-A, LOX-1, CD36.
体内研究
(In Vivo)

Inclisiran (1-10 mg/kg;腹腔注射;20 周) 可抑制高脂饮食诱发的动脉粥样硬化 ApoE-/- 小鼠中动脉粥样硬化的发展和细胞焦亡相关因子的表达[2]

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

Animal Model: Male ApoE-/- mice (8 weeks old, 17-20 g); high-fat diet (HFD)-induced atherosclerosis model[2]
Dosage: 1, 5, 10 mg/kg (dissolved in PBS)
Administration: Intraperitoneal injection; 20 weeks
Result: Significantly reduced LDL-C, TC, TG, and increased HDL-C in plasma.
Decreased aortic plaque area and lipid deposition.
Decreased pyroptosis-related factors (NLRP3, ASC, GSDMD, IL-1β, IL-18).
Clinical Trial
分子量

16339.00

CAS 号
性状

固体

颜色

White to off-white

Sequence

RNA, (Am-sp-(2'-deoxy-2'-fluoro)C-sp-Am-(2'-deoxy-2'-fluoro)A-(2'-deoxy-2'- fluoro)A-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)C-Am-(2'-deoxy-2'-fluoro)AAm-(2'-deoxy-2'-fluoro)A-Cm-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)G-Um-(2'-deoxy-2'-fluoro)C-Um-Am-Gm-sp-Am-sp-Am), complex with RNA (Cm-sp-Umsp -Am-Gm-Am-Cm-(2'-deoxy-2'-fluoro)C-Um-(2'-deoxy-2'-fluoro)G-Um-dT-UmUm-Gm-Cm-Um-Um-Um-Um-Gm-Um) 3'-[[(2S,4R)-1-[29-[[2-(acetylamino)-2- deoxy-β-D-galactopyranosyl]oxy]-14,14-bis[[3-[[3-[[5-[[2-(acetylamino)-2-deoxy-βD-galactopyranosyl]oxy]-1-oxopentyl]amino]propyl]amino]-3-oxopropoxy]methyl]- 1,12,19,25-tetraoxo-16-oxa-13,20,24-triazanonacos-1-yl]-4-hydroxy-2- pyrrolidinyl]methyl hydrogen phosphate] (1:1)

中文名称

英克司兰

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 5 mg/mL (0.31 mM; 超声助溶)

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
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浓度
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体积
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分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

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体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

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动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.80%

参考文献
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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产品名称:
Inclisiran
目录号:
HY-132591
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