1. Metabolic Enzyme/Protease Epigenetics Immunology/Inflammation Apoptosis 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 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).

For research use only. We do not sell to patients.

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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Based on 2 publication(s) in Google Scholar

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Description

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

 

In Vitro

Inclisiran (50-200 nM; 48 h) significantly inhibits cell death, cytotoxicity, and downregulates mRNA and protein expressions of pyroptosis-related factors in ox-LDL-induced HUVECs[2].
Inclisiran (50-200 nM; 48 h) inhibits ox-LDL-induced foam cell formation in Raw264.7 macrophages by activating the PPARγ pathway[3].

MedChemExpress (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.
In Vivo

Inclisiran (1-10 mg/kg; i.p.; 20 weeks) inhibits the development of atherosclerosis and pyroptosis-related factor expression in high-fat diet-induced atherosclerotic ApoE-/- mice[2].

MedChemExpress (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
Molecular Weight

16339.00

CAS No.
Appearance

Solid

Color

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)

SMILES

[Inclisiran]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

H2O : 5 mg/mL (0.31 mM; Need ultrasonic)

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Purity & Documentation

Purity: 99.80%

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  • 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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Inclisiran
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HY-132591
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